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ATP + a protein
ADP + a phosphoprotein
ATP + Bcl
ADP + phosphorylated Bcl
ATP + Bcl
ADP + phosphorylated Bcl10
-
Bcl10 is phosphorylated by the NEMO/IKK complex, recombinant substrate GST-Bcl10 expressed in HEK-293T cells, degradation of Bcl
-
-
?
ATP + Bcl10
ADP + phosphorylated Bcl10
-
negative regulatory activity of the IKK complex in Bcl10 degradation, which is part of the regulatory mechanisms that precisely control the response to antigens, overview
-
-
?
ATP + GST-IkappaBalpha
ADP + GST-IkappaBalpha phosphoprotein
-
activity assay
-
-
?
ATP + IkappaB alpha
ADP + phosphorylated IkappaB alpha
-
-
-
?
ATP + IkappaB protein
ADP + IkappaB phosphoprotein
-
-
-
-
?
ATP + IkappaB protein
ADP + phosphorylated IkappaB
-
the enzyme targets the inhibitory IkappaB protein tightly bound to the transcription factor NF-kappaB for proteasomal degradation and allows the freed NF-kappaB to enter the nucleus where it can be transactivate its target gene, IKKalpha is involved in inflammation in macrophages
-
-
?
ATP + IkappaBalpha
ADP + phosphorylated IkappaBalpha
ATP + IkappaBalpha
ADP + phosphorylated-IkappaBalpha
-
-
-
-
?
ATP + IkappaBbeta
ADP + phosphorylated IkappaBbeta
-
phosphorylation of IkappaBalpha at Ser19 and Ser23
-
-
?
ATP + interferon regulatory factor 3
ADP + phosphorylated interferon regulatory factor 3
-
-
-
?
ATP + KKKKERLLDDRHDSGLDSMKDEE
ADP + phosphorylated-KKKKERLLDDRHDSGLDSMKDEE
-
IKK substrate peptide derived from IkappaBalpha sequence
-
-
?
ATP + NF-kappaB
ADP + phosphorylated NF-kappaB
-
-
-
-
?
ATP + NF-kappaB p65 subunit
ADP + phosphorylated NF-kappaB p65 subunit
-
IKKalpha and IKKbeta phosphorylate NF-kappaB p65 subunit at Ser536
-
-
?
ATP + p65/RelA
ADP + phosphorylated p65/RelA
-
-
-
?
ATP + protein p100
ADP + phosphorylated protein p100
ATP + protein p165
ADP + phosphorylated protein p165
ATP + STAT1 transcription factor
ADP + phosphorylated STAT1 transcription factor
-
-
-
?
ATP + [acetylated histone H3 protein]
ADP + [acetylated histone H3 phosphoprotein]
ATP + [biotinylated IkappaBa peptide]
ADP + [biotinylated IkappaBa phosphopeptide]
i.e. biotin-Gly-Leu-Lys-Lys-Glu-Arg-Leu-Leu-Asp-Asp-Arg-His-Asp-Ser32-Gly-Leu-Asp-Ser36-Met-Lys-Asp-Glu-Glu
-
-
?
ATP + [DELTANp73alpha protein]
ADP + [DELTANp73alpha phosphoprotein]
-
phosphorylation at Ser422 by IKKbeta, IKKbeta is inactive with S422A mutant substrate. DELTANp73alpha i a dominant negative inhibitor of p53 and p73
-
-
?
ATP + [GST-IkappaB protein]
ADP + [GST-IkappaB phosphoprotein]
-
-
-
-
?
ATP + [GST-IkappaBalpha protein]
ADP + [GST-IkappaBalpha phosphoprotein]
-
-
-
-
?
ATP + [GST-IkappaBalpha1-54 protein]
ADP + [GST-IkappaBalpha1-54 phosphoprotein]
ATP + [GST-IkappaBbeta protein]
ADP + [GST-IkappaBbeta phosphoprotein]
-
-
-
-
?
ATP + [histone H3 protein]
ADP + [histone H3 phosphoprotein]
ATP + [IFN regulatory factor 3 protein (380-427)]
ADP + [IFN regulatory factor 3 phosphoprotein (380-427)]
-
the truncated mutant is a good substrate
-
-
?
ATP + [IFN regulatory factor 3 protein]
ADP + [IFN regulatory factor 3 phosphoprotein]
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
ATP + [IkappaBalpha protein]
ADP + [IkappaBalpha phosphoprotein]
ATP + [IkappaBbeta protein]
ADP + [IkappaBbeta phosphoprotein]
ATP + [IRF3 protein]
ADP + [IRF3 phosphoprotein]
-
phosphorylation at Ser396 by IKK-related IKKepsilon and TBK1 kinase
-
-
?
ATP + [leucine-rich repeat kinase 2 protein]
ADP + [leucine-rich repeat kinase 2 phosphoprotein]
ATP + [MYPT1]
ADP + [MYPT1 phosphoprotein]
the enzyme phosphorylates MYPT1 at Thr853
-
-
?
ATP + [NFkappaB subunit p56]
ADP + [NFkappaB subunit p56]phosphate
ATP + [optineurin protein]
ADP + [optineurin phosphoprotein]
-
phosphorylation at Ser177 by IKK-related IKKepsilon and TBK1 kinase
-
-
?
ATP + [p73 protein]
ADP + [p73 phosphoprotein]
-
IKKalpha in the nucleus
-
-
?
ATP + [RelA/p65 protein]
ADP + [RelA/p65 phosphoprotein]
ATP + [S386A IFN regulatory factor 3 protein]
ADP + [S386A IFN regulatory factor 3 phosphoprotein]
-
the mutant substrate is equally phosphorylated as the wild-type IRF3
-
-
?
ATP + [S396A IFN regulatory factor 3 protein]
ADP + [S396A IFN regulatory factor 3 phosphoprotein]
-
the mutant substrate is equally phosphorylated as the wild-type IRF3
-
-
?
ATP + [S402A/S404A/S405A IFN regulatory factor 3 protein]
ADP + [S402A/S404A/S405A IFN regulatory factor 3 phosphoprotein]
-
low activity with the IRF3 mutant
-
-
?
additional information
?
-
ATP + a protein
ADP + a phosphoprotein
CHUK associates with the NF-kappaB inhibitory protein, IkappaB-alpha, in mammalian cells. CHUK specifically phosphorylates IkappaB-alpha on both Ser32 and Ser36, modifications that are required for targeted degradation of IkappaB-alpha via the ubiquitin-proteasome pathway
-
-
?
ATP + a protein
ADP + a phosphoprotein
the I kappa B/NF-kappa B system is a key determinant of mucosal inflammation and protection
-
-
?
ATP + a protein
ADP + a phosphoprotein
phosphorylation of IkappaBs marks them out for destruction, thereby relieving their inhibitory effect on NF-kappaB
-
-
?
ATP + a protein
ADP + a phosphoprotein
phosphorylates IkappaB inhibitory proteins, causing their degradation and activation of transcription factor NF-kappaB, a master activator of inflammatory responses
-
-
?
ATP + a protein
ADP + a phosphoprotein
the I kappa B/NF-kappa B system is a key determinant of mucosal inflammation and protection
-
-
?
ATP + a protein
ADP + a phosphoprotein
phosphorylates IkappaB inhibitory proteins, causing their degradation and activation of transcription factor NF-kappaB, a master activator of inflammatory responses
-
-
?
ATP + a protein
ADP + a phosphoprotein
autophosphorylation at both Ser and Thr
-
-
?
ATP + a protein
ADP + a phosphoprotein
the expression of pkn1 is developmentally regulated to start immediately before spore formation. The enzyme plays an important role in the onset of proper differentiation
-
-
?
ATP + Bcl
ADP + phosphorylated Bcl
-
phosphorylation at the C-terminus of Bcl by IKKbeta disrupts Bcl10/Malt1 association and Bcl10-mediated signaling
-
-
?
ATP + Bcl
ADP + phosphorylated Bcl
-
phosphorylation at the C-terminus of Bcl by IKKbeta, inactive with a C-terminal 93 amino acid-deletion mutant of Bcl
-
-
?
ATP + Bcl
ADP + phosphorylated Bcl
-
phosphorylation at the C-terminus of Bcl by IKKbeta disrupts Bcl10/Malt1 association and Bcl10-mediated signaling
-
-
?
ATP + Bcl
ADP + phosphorylated Bcl
-
phosphorylation at the C-terminus of Bcl by IKKbeta, inactive with a C-terminal 93 amino acid-deletion mutant of Bcl
-
-
?
ATP + IkappaBalpha
ADP + phosphorylated IkappaBalpha
-
-
-
-
?
ATP + IkappaBalpha
ADP + phosphorylated IkappaBalpha
-
-
-
?
ATP + IkappaBalpha
ADP + phosphorylated IkappaBalpha
-
-
-
?
ATP + IkappaBalpha
ADP + phosphorylated IkappaBalpha
-
-
-
?
ATP + IkappaBalpha
ADP + phosphorylated IkappaBalpha
-
-
-
?
ATP + IkappaBalpha
ADP + phosphorylated IkappaBalpha
-
-
-
?
ATP + IkappaBalpha
ADP + phosphorylated IkappaBalpha
-
a step in NF-kappaB activation, the IKK complex, composed of IKKalpha, IKKbeta, and NEMO/IKKgamma, is the convergence point for many diverse NFkappaB-activating stimuli including TNFalpha, LPS, and IL-1, overview, IKKbeta is the primary positive regulator of NFkappaB activity in inflammatory processes, is the molecular link between inflammation and cancer
-
-
?
ATP + IkappaBalpha
ADP + phosphorylated IkappaBalpha
-
degradation of IkappaBalpha
-
-
?
ATP + IkappaBalpha
ADP + phosphorylated IkappaBalpha
-
recombinant GST-fusion substrate
-
-
?
ATP + IkappaBalpha
ADP + phosphorylated IkappaBalpha
phosphorylation at Ser-32 and Ser-36
-
-
?
ATP + IkappaBalpha
ADP + phosphorylated IkappaBalpha
-
phosphorylation of IkappaBalpha at Ser32 and Ser36
-
-
?
ATP + protein p100
ADP + phosphorylated protein p100
-
interaction with the NF-kappaB complex
-
-
?
ATP + protein p100
ADP + phosphorylated protein p100
-
required for the interaction with the NF-kappaB complex
-
-
?
ATP + protein p165
ADP + phosphorylated protein p165
-
p65 is part of the IKKepsilon complex with p25, interaction with the NF-kappaB complex
-
-
?
ATP + protein p165
ADP + phosphorylated protein p165
-
required for the interaction with the NF-kappaB complex
-
-
?
ATP + [acetylated histone H3 protein]
ADP + [acetylated histone H3 phosphoprotein]
-
IKKalpha is required for histone function regulation in the nucleus
-
-
?
ATP + [acetylated histone H3 protein]
ADP + [acetylated histone H3 phosphoprotein]
-
phosphorylation at Ser10
-
-
?
ATP + [acetylated histone H3 protein]
ADP + [acetylated histone H3 phosphoprotein]
-
IKKalpha is required for histone function regulation in the nucleus
-
-
?
ATP + [acetylated histone H3 protein]
ADP + [acetylated histone H3 phosphoprotein]
-
phosphorylation at Ser10
-
-
?
ATP + [GST-IkappaBalpha1-54 protein]
ADP + [GST-IkappaBalpha1-54 phosphoprotein]
-
-
-
-
?
ATP + [GST-IkappaBalpha1-54 protein]
ADP + [GST-IkappaBalpha1-54 phosphoprotein]
-
-
-
-
?
ATP + [GST-IkappaBalpha1-54 protein]
ADP + [GST-IkappaBalpha1-54 phosphoprotein]
-
recombinant substrate derived from mouse IkappaBalpha
-
-
?
ATP + [histone H3 protein]
ADP + [histone H3 phosphoprotein]
-
-
-
-
?
ATP + [histone H3 protein]
ADP + [histone H3 phosphoprotein]
-
histone H3 phosphorylation by IKK-alpha is critical for cytokine-induced gene expression
-
-
?
ATP + [histone H3 protein]
ADP + [histone H3 phosphoprotein]
-
histone H3 phosphorylation by IKK-alpha is critical for cytokine-induced gene expression
-
-
?
ATP + [histone H3 protein]
ADP + [histone H3 phosphoprotein]
-
phosphorylation at Ser10 by IKK-alpha
-
-
?
ATP + [IFN regulatory factor 3 protein]
ADP + [IFN regulatory factor 3 phosphoprotein]
-
IRF3 activation is triggered by IKKepsilon/TBK1-mediated phosphorylation on Ser396
-
-
?
ATP + [IFN regulatory factor 3 protein]
ADP + [IFN regulatory factor 3 phosphoprotein]
-
phosphorylation on Ser396, and phosphorylation of Ser402/404/405 cluster in the C-terminal regulatory domain of IRF3 in vitro
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
-
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
-
661346, 661547, 662155, 662516, 662684, 662847, 662942, 663441, 702333, 702590, 703253, 703737, 704348, 704783, 705026, 705033, 705074, 705320, 722119, 722826, 723174, 738780, 739047, 739219 -
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
signalling step of IKK bound to NFkappaB for subsequent ubiquitination of IkappaB and proteolytic degradation
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
the enzyme is also active with a peptide derived from IkappaB protein spanning Ser32 and Ser36 which are phosphorylated
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
the IkappaBalpha subunit of NF-kappaB is phosphorylated at serine residues 32 and 36
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
phosphorylation at Ser32 and Ser36 catalyzed by IkappaBalpha kinase
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
-
661559, 662500, 662516, 662570, 662731, 662931, 662942, 663395, 663441, 703140, 704912, 705074, 705320, 705662, 722119, 722826 -
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
inhibition and degradation of IkappaB, an inhibitor of NF-kappaB retaining it in the cytoplasm, phosphorylation of IkappaB marks the protein for ubiquitination followed by degradation, activated NF-kappaB is translocated to the nucleus initiating signalling pathways, regulation mechanism, overview
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
inhibitor substrate is bound to NF-kappaB
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
phosphorylation of IkappaB results in its proteolytic degradation
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
required for activation of NF-kappaB resulting in activation of signalling pathways
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
-
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
-
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
parasite IKKalpha, localized in parasitophorous vacuole membrane, activates mouse' intracellular NF-kappaB in early infection stage resulting in NF-kappaB nuclear translocation and subsequent gene expression independently from the host IKK complex
-
-
?
ATP + [IkappaBalpha protein]
ADP + [IkappaBalpha phosphoprotein]
-
-
-
-
?
ATP + [IkappaBalpha protein]
ADP + [IkappaBalpha phosphoprotein]
-
enzyme is involved in activation of pro-inflammation signalling
-
-
?
ATP + [IkappaBalpha protein]
ADP + [IkappaBalpha phosphoprotein]
-
phosphorylation at Ser32 and Ser36
-
-
?
ATP + [IkappaBalpha protein]
ADP + [IkappaBalpha phosphoprotein]
-
IKKbeta-dependent phosphorylation and subsequent ubiquitin-dependent proteolytic degradation of IKKalpha, the 2 subunits have opposing function in NF-kappaB metabolism, overview
-
-
?
ATP + [IkappaBalpha protein]
ADP + [IkappaBalpha phosphoprotein]
-
phosphorylation at Ser32 and Ser36
-
-
?
ATP + [IkappaBalpha protein]
ADP + [IkappaBalpha phosphoprotein]
-
phosphorylation on Ser32 and Ser36
-
-
?
ATP + [IkappaBalpha protein]
ADP + [IkappaBalpha phosphoprotein]
-
parasite IKKalpha, localized in parasitophorous vacuole membrane, activates mouse' intracellular NF-kappaB through phosphorylation of host IkappaBalpha at Ser32 and Ser36 in early infection stage resulting in NF-kappaB nuclear translocation and subsequent gene expression independently from the host IKK complex
-
-
?
ATP + [IkappaBbeta protein]
ADP + [IkappaBbeta phosphoprotein]
-
-
-
-
?
ATP + [IkappaBbeta protein]
ADP + [IkappaBbeta phosphoprotein]
-
phosphorylation at Ser19 and Ser23
-
-
?
ATP + [IkappaBbeta protein]
ADP + [IkappaBbeta phosphoprotein]
-
phosphorylation at Ser19 and Ser23
-
-
?
ATP + [leucine-rich repeat kinase 2 protein]
ADP + [leucine-rich repeat kinase 2 phosphoprotein]
-
catalyzed reaction of canonical IKKalpha and IKKbeta and IKK-related IKKepsilon and TBK1 kinase
-
-
?
ATP + [leucine-rich repeat kinase 2 protein]
ADP + [leucine-rich repeat kinase 2 phosphoprotein]
-
phosphorylation of LRRK2 at Ser910 and Ser935 by IKKalpha and IKKbeta
-
-
?
ATP + [NFkappaB subunit p56]
ADP + [NFkappaB subunit p56]phosphate
-
-
-
-
?
ATP + [NFkappaB subunit p56]
ADP + [NFkappaB subunit p56]phosphate
-
phosphorylation at serine residues, especially at S536, in the cytoplasm prior to NFkappaB p56 translocation to the nucleus
-
-
?
ATP + [RelA/p65 protein]
ADP + [RelA/p65 phosphoprotein]
-
-
-
-
?
ATP + [RelA/p65 protein]
ADP + [RelA/p65 phosphoprotein]
-
phosphorylation on Ser536 of the transactivation domain, dependent on lipopolysaccharide-induction, but not on Akt or p65
-
-
?
additional information
?
-
-
activation of heterodimeric nuclear transcription factor NFkappaB is an essential step in inflammation, e.g. resulting in osteoarthritis, ulcerative colitis, asthma, and Crohn's disease, signalling step for phosphorylation, subsequent ubiquitination and proteolytic degradation of IkappaB, NFkappaB remains free after the reaction and is translocated to the nucleus, NFkappaB activation is also involved in development of diseases like cancer, gut ischemia-reperfusion, diabetes, or in transplant rejections, overview
-
-
?
additional information
?
-
-
defective ubiquination of the NF-kappaB essential modifier/IkappaB kinase-gamma complex leads to impaired cellular NFkappaB signalling and hypohidrotic ectodermal dysplasia with immunodeficiency HED-ID
-
-
?
additional information
?
-
-
enzyme is responsible for NFkappaB activation, specific inhibition of IkB kinase reduces hyperalgesia in inflammatory and neuropathic pain models in male Sprague-Dawley rats
-
-
?
additional information
?
-
-
IKK activates and regulates NFkappaB important in intracellular signalling, overview
-
-
?
additional information
?
-
-
IKK activates NF-kappaB through action of TNFalpha playing an important role in subsequent signaling pathways involved in e.g. apoptosis/cell survival, cell proliferation, and inflammation
-
-
?
additional information
?
-
-
IKK activates NF-kappaB which initiates signaling pathways that play critical roles in a variety of physiological and pathological processes, e.g. promotion of cell survival inducing production of apoptosis inhibitors in normal and cancer cells, pathways overview, IKK/NF-kappaB links inflammation to cancer, regulation of IKK, overview
-
-
?
additional information
?
-
-
IKK activates TNFalpha-dependent signaling pathways inducing 5-fluoro-2'-deoxyuridine drug resistance in different cell lines, overview
-
-
?
additional information
?
-
-
IKK is responsible for activation of NFkappaB, herpesvirus HSV-1 potently induces IkappaB kinase IKK causing persistent induction of NFkappaB resulting in transactivation of HIV-1-LTR-regulated genes and induction of HIV-1 replication in infected T-cells
-
-
?
additional information
?
-
-
IKK marks cytoplasmic NFkappaB inhibitors for proteolytic destruction playing a role in regulation of genetic cell cycle programs, IKK regulates nuclear translocation of transcription factor NFkappaB
-
-
?
additional information
?
-
-
IKKalpha, not IKKbeta, is required for epidermal regeneration, IkappaB kinases are essential key regulators of the canonical and noncanonical NFkappaB pathways important for the expression of a wide variety of genes that are involved in the control of immune and inflammatory response, and in the regulation of cellular proliferation and survival, mechanism, overview
-
-
?
additional information
?
-
-
IKKbeta regulates the translocation of NF-kappaB from cytoplasm to nucleus earmarking the transcription factor for polyubiquitination and proteasome-mediated degradation, the cytokine TNFalpha-induced T-loop-phosphorylated IKKbeta becomes monoubiquitinated at Lyk163 proximal to the T-loop, mechanism of post-translational crosstalk, overview
-
-
?
additional information
?
-
-
infection and genome insertion of human cytomegalovirus induces expression of the catalytic subunit IKK2 in the host cell which is required for viral induction of NF-kappaB activation and involved in viral replication and lytic cycle
-
-
?
additional information
?
-
-
the IKK complex is responsible for NFkappaB regulation
-
-
?
additional information
?
-
-
the noncanonical IkappaB kinase homologue IKKepsilon, beneath TANK-binding kinase-1 TBK-1, is required for activation of transcription factor NFkappaB and of interferon regulatory factor 3 IRF3, regulation and interaction, overview
-
-
?
additional information
?
-
-
Vav-1 and IKKalpha subunit of IkappaB kinase functionally associate to induce NFkappaB activation in response to CD28 engagement
-
-
?
additional information
?
-
-
TNF-R1-activated IKKbeta phosphorylates IKKgamma and IKKalpha, autophosphorylation patterns involving K163 of IKKbeta, regulation, overview
-
-
?
additional information
?
-
-
hypoxia alters the cellular pool of IKKalpha and IKKbeta, and activates NFkappaB through a pathway involving activation of IkappaB kinase-beta, IKKbeta, leading to phosphorylation-dependent degradation of IkappaBalpha and liberation of NFkappaB, overview, hypoxia-induced activation of the NFkappaB pathway is independent of HIF-1alpha, prolyl hydroxylase-1 negatively regulates IKKbeta
-
-
?
additional information
?
-
-
IkappaB kinase beta plays an essential role in remodeling Carma1-Bcl10-Malt1 complexes upon T cell activation, T cell receptor signaling to IkappaB kinase/NF-kappaB is controlled by PKCtheta-dependent activation of the Carma1, Bcl10, and Malt1 CBM complex, IKKbeta triggers the CBM complex formation and phosphorylation of Bcl by PMA/ionomycin or CD3/CD28, regulation, overview
-
-
?
additional information
?
-
-
IKK is responsible for activation of NF-kappaB by initiating the degradation of the NF-kappaB inhibitor IkappaB, subunits IKKalpha and IKKgamma/NEMO, not IKKbeta, are required for reovirus-induced NF-kappaB activation and apoptosis, overview
-
-
?
additional information
?
-
-
IKK-beta inhibition in vivo leads to reduction of rhinovirus-induced expression of CXCL8, CCL5, and IL-6, the enzyme is important in regulation of the NF-kappaB signaling pathway, overview
-
-
?
additional information
?
-
-
IKKalpha and IKKbeta are distinctly involved in ERK1-dependent, but IkappaBalpha-P65- and p100-p52-independent, upregulation of MUC5AC mucin transcription in case of infection by Streptococcus pneumoniae, MUC5AC mucin induction also requires pneumolysin and TLR4-dependent MyD88-IRAK1-TRAF6 signaling, molecular mechanism, overview
-
-
?
additional information
?
-
-
IKKbeta subunit of IKK complex is essential for the activation of NF-kappaB in response to various proinflammatory signals, Cys179 of IkappaB kinase beta plays a critical role in enzyme activation by promoting phosphorylation of activation loop serines, overview
-
-
?
additional information
?
-
-
no activity with Rip2
-
-
?
additional information
?
-
-
activation of NFkappaB by the catalytic subunit IKKbeta is required for signaling via the NFkappaB pathway in acute and systemic inflammation and for tissue protection
-
-
?
additional information
?
-
-
IkappaB kinases are essential key regulators of the NFkappaB pathways in the tooth development acting as stimulators, overview
-
-
?
additional information
?
-
-
IKK activates NF-kappaB which initiates signaling pathways that play critical roles in a variety of physiological and pathological processes, e.g. promotion of cell survival inducing production of apoptosis inhibitors in normal and cancer cells, pathways overview, IKK/NF-kappaB links inflammation to cancer, regulation of IKK, overview
-
-
?
additional information
?
-
-
IKK is involved in NF-kappaB activation, IkappaB kinase IKKbeta, but not IKKalpha, is a critical mediator of NF-kappaB-dependent osteoclast survival preventing TNFalpha-induced cell death, and is required for formation of fully functional bone-resorbing osteoclasts and for inflammation-induced bone loss
-
-
?
additional information
?
-
-
IKK is required for activation of NF-kappaB and subsequent signalling pathways
-
-
?
additional information
?
-
-
IKK is responsible for NF-kappaB activation by inactivating its inhibitor IkappaB, different inflammation stimuli induce distinct IKK activity profiles, molecular mechanism, overview
-
-
?
additional information
?
-
-
IKKalpha, not IKKbeta, is required for epidermal regeneration, IkappaB kinases are essential key regulators of the canonical and noncanonical NFkappaB pathways important for the expression of a wide variety of genes that are involved in the control of immune and inflammatory response, and in the regulation of cellular proliferation and survival, mechanism, overview
-
-
?
additional information
?
-
-
IKKbeta is required for activation of NFkappaB, IKKbeta induces expression of epithelial sodium channel alphabetagamma-ENaC in cell surfaces
-
-
?
additional information
?
-
-
IKKbeta is required for regulation of NFkappaB activity and peripheral B cell survival and proliferation
-
-
?
additional information
?
-
-
parasite Toxoplasma gondii IKKalpha, localized in parasitophorous vacuole membrane, activates the host intracellular NF-kappaB in early infection stage resulting in NF-kappaB nuclear translocation and subsequent gene expression independently from the host IKK complex
-
-
?
additional information
?
-
-
subunit IKKbeta controls the activation of NF-kappaB, important in inflammation, IKKalpha plays a role in lyphoid organogenesis and suppresses NF-kappaB activity by accelerating both the turnover of the NFkappaB subunits RelA and c-Rel, and their removal from pro-inflammatory gene promoters, inactivation of IKKalpha enhances inflammation and bacterial clearance in mice, overview
-
-
?
additional information
?
-
-
activated IKK2 is responsible for induction of leucocyte infiltration in pancreatic acini, the mutant ICC2CA in pancreatic acinar cells increases tissue damage of secretagogue induced experimental pancreatitits, the enzyme is involved in the proinflammatory IKK/NF-kappaB pathway, overview
-
-
?
additional information
?
-
-
IkappaB kinase beta plays a critical role in metallothionein-1 expression and protection against arsenic toxicity, two signaling pathways appear to be important for modulating arsenic toxicity. First, the IKK-NF-kappaB pathway is crucial for maintaining cellular metallothionein-1 levels to counteract reactive oxygen species accumulation, and second, when this pathway fails, excessive reactive oxygen species leads to activation of the MKK4-JNK pathway, resulting in apoptosis
-
-
?
additional information
?
-
-
IkappaB kinase beta plays an essential role in remodeling Carma1-Bcl10-Malt1 complexes upon T cell activation, T cell receptor signaling to IkappaB kinase/NF-kappaB is controlled by PKCtheta-dependent activation of the Carma1, Bcl10, and Malt1 CBM complex, IKKbeta triggers the CBM complex formation and phosphorylation of Bcl by PMA/ionomycin or CD3/CD28, regulation, overview
-
-
?
additional information
?
-
-
IkappaB kinase-alpha is critical for interferon-alpha production induced by Toll-like receptors 7 and 9, but IKK-a is dispensable for a cytoplasmic RNA helicase RIG-I-dependent cytosolic pathway-induced production of IFN-alpha in MEF cells, overview
-
-
?
additional information
?
-
-
IKK-related kinases tank-binding kinase 1 TBK1/IKKi and cullin-based ubiquitin ligases are involved in IFN regulatory factor-3, IRF-3, phosphorylation, activation, and degradation, IRF-3 activation is induced by viral infection, e.g. by HCMV, molecular mechanisms, detailed overview
-
-
?
additional information
?
-
-
IKKalpha and IKKbeta are distinctly involved in ERK1-dependent, but IkappaBalpha-P65- and p100-p52-independent, upregulation of MUC5AC mucin transcription in case of infection by Streptococcus pneumoniae, MUC5AC mucin induction also requires pneumolysin and TLR4-dependent MyD88-IRAK1-TRAF6 signaling, molecular mechanism, overview
-
-
?
additional information
?
-
-
IKKalpha enhances p73-mediated transactivation and pro-apoptotic functions in p53-deficient H1299 cells, stabilization of p73, but not of the antagonist p53, by nuclear IKKalpha mediates cisplatin-induced apoptosis, DNA damage-induced accumulation of both p53 and p73alpha is associated with the up-regulation of IKK-alpha and IKK-gamma, a functional interaction might exist between them in DNA damage-mediated apoptotic pathways
-
-
?
additional information
?
-
-
IKKalpha is involved in the noncanonical NF-kappaB activation pathway, and plays an essential role in thymic organogenesis required for the establishment of self-tolerance, overview
-
-
?
additional information
?
-
-
IKKalpha is not only a regulator of mammary epithelial proliferation, but is also an important contributor to ErbB2-induced oncogenesis, providing signals that maintain mammary tumor-initiating cells, IKKalpha activity is required for cyclin D1 induction and proliferation of lobuloalveolar epithelial cells, and is required for self-renewal of ErbB2/Her2-transformed mammary tumor-initiating cells, overview
-
-
?
additional information
?
-
-
IKKepsilon is important in the regulation of the alternative NF-kappaB activation pathway involving p52 and p65, IKKepsilon interacts with p52 and promotes transactivation via p65
-
-
?
additional information
?
-
-
IKKepsilon, i.e. IKKi, is implicated in virus induction of interferon-beta, IFNbeta, and development of immunity, IKKepsilon functions in a redundant role to its ubiquitous counterpart, TBK1, in the activation of IRF3 and IRF7 ex vivo, IKKe determines ISGF3 binding specificity, regulaiton, overview
-
-
?
additional information
?
-
-
mechanisms/pathways of activation and derepression of the IKK complex, regulation, detailed overview
-
-
?
additional information
?
-
-
IKKalpha interacts with p73
-
-
?
additional information
?
-
-
interaction analysis of IKKepsilon with NF-kappaB complex components/p25/p65 by immunoprecipitation and mass spectrometric analysis, overview
-
-
?
additional information
?
-
-
the enzyme activity is included in a complex formed of the scaffold protein NF-kappaB essential modulator, i.e. NEMO or IKKgamma, and the Ikkalpha and IKKbeta kinases, overview
-
-
?
additional information
?
-
-
IKKalpha and IKKbeta are distinctly involved in ERK1-dependent, but IkappaBalpha-P65- and p100-p52-independent, upregulation of MUC5AC mucin transcription in case of infection by Streptococcus pneumoniae, MUC5AC mucin induction also requires pneumolysin and TLR4-dependent MyD88-IRAK1-TRAF6 signaling, molecular mechanism, overview
-
-
?
additional information
?
-
-
activation of NFkappaB by the catalytic subunit IKKbeta is required for signaling via the NFkappaB pathway in acute and systemic inflammation and for tissue protection
-
-
?
additional information
?
-
-
the IkappaB kinase regulates chromatin structure during reconsolidation of conditioned fear memories, IKKalpha is involved in the regulation of histone H3 phosphorylation and acetylation at specific gene promoters in hippocampus in the NF-kappaB pathway, inhibition of IKKalpha regulation results in impairments in fear memory reconsolidation, mechanism, overview
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?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
ATP + a protein
ADP + a phosphoprotein
ATP + Bcl
ADP + phosphorylated Bcl
ATP + Bcl10
ADP + phosphorylated Bcl10
-
negative regulatory activity of the IKK complex in Bcl10 degradation, which is part of the regulatory mechanisms that precisely control the response to antigens, overview
-
-
?
ATP + IkappaB protein
ADP + phosphorylated IkappaB
-
the enzyme targets the inhibitory IkappaB protein tightly bound to the transcription factor NF-kappaB for proteasomal degradation and allows the freed NF-kappaB to enter the nucleus where it can be transactivate its target gene, IKKalpha is involved in inflammation in macrophages
-
-
?
ATP + IkappaBalpha
ADP + phosphorylated IkappaBalpha
ATP + NF-kappaB
ADP + phosphorylated NF-kappaB
-
-
-
-
?
ATP + protein p100
ADP + phosphorylated protein p100
-
interaction with the NF-kappaB complex
-
-
?
ATP + protein p165
ADP + phosphorylated protein p165
-
p65 is part of the IKKepsilon complex with p25, interaction with the NF-kappaB complex
-
-
?
ATP + [acetylated histone H3 protein]
ADP + [acetylated histone H3 phosphoprotein]
ATP + [GST-IkappaB protein]
ADP + [GST-IkappaB phosphoprotein]
-
-
-
-
?
ATP + [GST-IkappaBalpha protein]
ADP + [GST-IkappaBalpha phosphoprotein]
-
-
-
-
?
ATP + [histone H3 protein]
ADP + [histone H3 phosphoprotein]
ATP + [IFN regulatory factor 3 protein]
ADP + [IFN regulatory factor 3 phosphoprotein]
-
IRF3 activation is triggered by IKKepsilon/TBK1-mediated phosphorylation on Ser396
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
ATP + [IkappaBalpha protein]
ADP + [IkappaBalpha phosphoprotein]
ATP + [IkappaBbeta protein]
ADP + [IkappaBbeta phosphoprotein]
-
-
-
-
?
ATP + [IRF3 protein]
ADP + [IRF3 phosphoprotein]
-
phosphorylation at Ser396 by IKK-related IKKepsilon and TBK1 kinase
-
-
?
ATP + [leucine-rich repeat kinase 2 protein]
ADP + [leucine-rich repeat kinase 2 phosphoprotein]
-
catalyzed reaction of canonical IKKalpha and IKKbeta and IKK-related IKKepsilon and TBK1 kinase
-
-
?
ATP + [MYPT1]
ADP + [MYPT1 phosphoprotein]
the enzyme phosphorylates MYPT1 at Thr853
-
-
?
ATP + [NFkappaB subunit p56]
ADP + [NFkappaB subunit p56]phosphate
-
-
-
-
?
ATP + [optineurin protein]
ADP + [optineurin phosphoprotein]
-
phosphorylation at Ser177 by IKK-related IKKepsilon and TBK1 kinase
-
-
?
ATP + [p73 protein]
ADP + [p73 phosphoprotein]
-
IKKalpha in the nucleus
-
-
?
ATP + [RelA/p65 protein]
ADP + [RelA/p65 phosphoprotein]
-
-
-
-
?
additional information
?
-
ATP + a protein
ADP + a phosphoprotein
CHUK associates with the NF-kappaB inhibitory protein, IkappaB-alpha, in mammalian cells. CHUK specifically phosphorylates IkappaB-alpha on both Ser32 and Ser36, modifications that are required for targeted degradation of IkappaB-alpha via the ubiquitin-proteasome pathway
-
-
?
ATP + a protein
ADP + a phosphoprotein
the I kappa B/NF-kappa B system is a key determinant of mucosal inflammation and protection
-
-
?
ATP + a protein
ADP + a phosphoprotein
phosphorylation of IkappaBs marks them out for destruction, thereby relieving their inhibitory effect on NF-kappaB
-
-
?
ATP + a protein
ADP + a phosphoprotein
phosphorylates IkappaB inhibitory proteins, causing their degradation and activation of transcription factor NF-kappaB, a master activator of inflammatory responses
-
-
?
ATP + a protein
ADP + a phosphoprotein
the I kappa B/NF-kappa B system is a key determinant of mucosal inflammation and protection
-
-
?
ATP + a protein
ADP + a phosphoprotein
phosphorylates IkappaB inhibitory proteins, causing their degradation and activation of transcription factor NF-kappaB, a master activator of inflammatory responses
-
-
?
ATP + a protein
ADP + a phosphoprotein
the expression of pkn1 is developmentally regulated to start immediately before spore formation. The enzyme plays an important role in the onset of proper differentiation
-
-
?
ATP + Bcl
ADP + phosphorylated Bcl
-
phosphorylation at the C-terminus of Bcl by IKKbeta disrupts Bcl10/Malt1 association and Bcl10-mediated signaling
-
-
?
ATP + Bcl
ADP + phosphorylated Bcl
-
phosphorylation at the C-terminus of Bcl by IKKbeta disrupts Bcl10/Malt1 association and Bcl10-mediated signaling
-
-
?
ATP + IkappaBalpha
ADP + phosphorylated IkappaBalpha
-
-
-
-
?
ATP + IkappaBalpha
ADP + phosphorylated IkappaBalpha
-
a step in NF-kappaB activation, the IKK complex, composed of IKKalpha, IKKbeta, and NEMO/IKKgamma, is the convergence point for many diverse NFkappaB-activating stimuli including TNFalpha, LPS, and IL-1, overview, IKKbeta is the primary positive regulator of NFkappaB activity in inflammatory processes, is the molecular link between inflammation and cancer
-
-
?
ATP + IkappaBalpha
ADP + phosphorylated IkappaBalpha
-
degradation of IkappaBalpha
-
-
?
ATP + [acetylated histone H3 protein]
ADP + [acetylated histone H3 phosphoprotein]
-
IKKalpha is required for histone function regulation in the nucleus
-
-
?
ATP + [acetylated histone H3 protein]
ADP + [acetylated histone H3 phosphoprotein]
-
IKKalpha is required for histone function regulation in the nucleus
-
-
?
ATP + [histone H3 protein]
ADP + [histone H3 phosphoprotein]
-
-
-
-
?
ATP + [histone H3 protein]
ADP + [histone H3 phosphoprotein]
-
histone H3 phosphorylation by IKK-alpha is critical for cytokine-induced gene expression
-
-
?
ATP + [histone H3 protein]
ADP + [histone H3 phosphoprotein]
-
histone H3 phosphorylation by IKK-alpha is critical for cytokine-induced gene expression
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
-
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
-
661346, 662155, 662516, 662684, 662847, 662942, 663441, 702333, 702590, 703253, 703737, 704348, 704783, 705026, 705033, 705074, 705320, 722119, 722826, 723174, 738780, 739047, 739219 -
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
signalling step of IKK bound to NFkappaB for subsequent ubiquitination of IkappaB and proteolytic degradation
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
the IkappaBalpha subunit of NF-kappaB is phosphorylated at serine residues 32 and 36
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
-
661559, 662516, 662570, 662942, 663441, 703140, 704912, 705074, 705320, 705662, 722119, 722826 -
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
inhibition and degradation of IkappaB, an inhibitor of NF-kappaB retaining it in the cytoplasm, phosphorylation of IkappaB marks the protein for ubiquitination followed by degradation, activated NF-kappaB is translocated to the nucleus initiating signalling pathways, regulation mechanism, overview
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
inhibitor substrate is bound to NF-kappaB
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
phosphorylation of IkappaB results in its proteolytic degradation
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
required for activation of NF-kappaB resulting in activation of signalling pathways
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
-
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
-
parasite IKKalpha, localized in parasitophorous vacuole membrane, activates mouse' intracellular NF-kappaB in early infection stage resulting in NF-kappaB nuclear translocation and subsequent gene expression independently from the host IKK complex
-
-
?
ATP + [IkappaBalpha protein]
ADP + [IkappaBalpha phosphoprotein]
-
-
-
-
?
ATP + [IkappaBalpha protein]
ADP + [IkappaBalpha phosphoprotein]
-
enzyme is involved in activation of pro-inflammation signalling
-
-
?
ATP + [IkappaBalpha protein]
ADP + [IkappaBalpha phosphoprotein]
-
parasite IKKalpha, localized in parasitophorous vacuole membrane, activates mouse' intracellular NF-kappaB through phosphorylation of host IkappaBalpha at Ser32 and Ser36 in early infection stage resulting in NF-kappaB nuclear translocation and subsequent gene expression independently from the host IKK complex
-
-
?
additional information
?
-
-
activation of heterodimeric nuclear transcription factor NFkappaB is an essential step in inflammation, e.g. resulting in osteoarthritis, ulcerative colitis, asthma, and Crohn's disease, signalling step for phosphorylation, subsequent ubiquitination and proteolytic degradation of IkappaB, NFkappaB remains free after the reaction and is translocated to the nucleus, NFkappaB activation is also involved in development of diseases like cancer, gut ischemia-reperfusion, diabetes, or in transplant rejections, overview
-
-
?
additional information
?
-
-
defective ubiquination of the NF-kappaB essential modifier/IkappaB kinase-gamma complex leads to impaired cellular NFkappaB signalling and hypohidrotic ectodermal dysplasia with immunodeficiency HED-ID
-
-
?
additional information
?
-
-
enzyme is responsible for NFkappaB activation, specific inhibition of IkB kinase reduces hyperalgesia in inflammatory and neuropathic pain models in male Sprague-Dawley rats
-
-
?
additional information
?
-
-
IKK activates and regulates NFkappaB important in intracellular signalling, overview
-
-
?
additional information
?
-
-
IKK activates NF-kappaB through action of TNFalpha playing an important role in subsequent signaling pathways involved in e.g. apoptosis/cell survival, cell proliferation, and inflammation
-
-
?
additional information
?
-
-
IKK activates NF-kappaB which initiates signaling pathways that play critical roles in a variety of physiological and pathological processes, e.g. promotion of cell survival inducing production of apoptosis inhibitors in normal and cancer cells, pathways overview, IKK/NF-kappaB links inflammation to cancer, regulation of IKK, overview
-
-
?
additional information
?
-
-
IKK activates TNFalpha-dependent signaling pathways inducing 5-fluoro-2'-deoxyuridine drug resistance in different cell lines, overview
-
-
?
additional information
?
-
-
IKK is responsible for activation of NFkappaB, herpesvirus HSV-1 potently induces IkappaB kinase IKK causing persistent induction of NFkappaB resulting in transactivation of HIV-1-LTR-regulated genes and induction of HIV-1 replication in infected T-cells
-
-
?
additional information
?
-
-
IKK marks cytoplasmic NFkappaB inhibitors for proteolytic destruction playing a role in regulation of genetic cell cycle programs, IKK regulates nuclear translocation of transcription factor NFkappaB
-
-
?
additional information
?
-
-
IKKalpha, not IKKbeta, is required for epidermal regeneration, IkappaB kinases are essential key regulators of the canonical and noncanonical NFkappaB pathways important for the expression of a wide variety of genes that are involved in the control of immune and inflammatory response, and in the regulation of cellular proliferation and survival, mechanism, overview
-
-
?
additional information
?
-
-
IKKbeta regulates the translocation of NF-kappaB from cytoplasm to nucleus earmarking the transcription factor for polyubiquitination and proteasome-mediated degradation, the cytokine TNFalpha-induced T-loop-phosphorylated IKKbeta becomes monoubiquitinated at Lyk163 proximal to the T-loop, mechanism of post-translational crosstalk, overview
-
-
?
additional information
?
-
-
infection and genome insertion of human cytomegalovirus induces expression of the catalytic subunit IKK2 in the host cell which is required for viral induction of NF-kappaB activation and involved in viral replication and lytic cycle
-
-
?
additional information
?
-
-
the IKK complex is responsible for NFkappaB regulation
-
-
?
additional information
?
-
-
the noncanonical IkappaB kinase homologue IKKepsilon, beneath TANK-binding kinase-1 TBK-1, is required for activation of transcription factor NFkappaB and of interferon regulatory factor 3 IRF3, regulation and interaction, overview
-
-
?
additional information
?
-
-
Vav-1 and IKKalpha subunit of IkappaB kinase functionally associate to induce NFkappaB activation in response to CD28 engagement
-
-
?
additional information
?
-
-
hypoxia alters the cellular pool of IKKalpha and IKKbeta, and activates NFkappaB through a pathway involving activation of IkappaB kinase-beta, IKKbeta, leading to phosphorylation-dependent degradation of IkappaBalpha and liberation of NFkappaB, overview, hypoxia-induced activation of the NFkappaB pathway is independent of HIF-1alpha, prolyl hydroxylase-1 negatively regulates IKKbeta
-
-
?
additional information
?
-
-
IkappaB kinase beta plays an essential role in remodeling Carma1-Bcl10-Malt1 complexes upon T cell activation, T cell receptor signaling to IkappaB kinase/NF-kappaB is controlled by PKCtheta-dependent activation of the Carma1, Bcl10, and Malt1 CBM complex, IKKbeta triggers the CBM complex formation and phosphorylation of Bcl by PMA/ionomycin or CD3/CD28, regulation, overview
-
-
?
additional information
?
-
-
IKK is responsible for activation of NF-kappaB by initiating the degradation of the NF-kappaB inhibitor IkappaB, subunits IKKalpha and IKKgamma/NEMO, not IKKbeta, are required for reovirus-induced NF-kappaB activation and apoptosis, overview
-
-
?
additional information
?
-
-
IKK-beta inhibition in vivo leads to reduction of rhinovirus-induced expression of CXCL8, CCL5, and IL-6, the enzyme is important in regulation of the NF-kappaB signaling pathway, overview
-
-
?
additional information
?
-
-
IKKalpha and IKKbeta are distinctly involved in ERK1-dependent, but IkappaBalpha-P65- and p100-p52-independent, upregulation of MUC5AC mucin transcription in case of infection by Streptococcus pneumoniae, MUC5AC mucin induction also requires pneumolysin and TLR4-dependent MyD88-IRAK1-TRAF6 signaling, molecular mechanism, overview
-
-
?
additional information
?
-
-
IKKbeta subunit of IKK complex is essential for the activation of NF-kappaB in response to various proinflammatory signals, Cys179 of IkappaB kinase beta plays a critical role in enzyme activation by promoting phosphorylation of activation loop serines, overview
-
-
?
additional information
?
-
-
activation of NFkappaB by the catalytic subunit IKKbeta is required for signaling via the NFkappaB pathway in acute and systemic inflammation and for tissue protection
-
-
?
additional information
?
-
-
IkappaB kinases are essential key regulators of the NFkappaB pathways in the tooth development acting as stimulators, overview
-
-
?
additional information
?
-
-
IKK activates NF-kappaB which initiates signaling pathways that play critical roles in a variety of physiological and pathological processes, e.g. promotion of cell survival inducing production of apoptosis inhibitors in normal and cancer cells, pathways overview, IKK/NF-kappaB links inflammation to cancer, regulation of IKK, overview
-
-
?
additional information
?
-
-
IKK is involved in NF-kappaB activation, IkappaB kinase IKKbeta, but not IKKalpha, is a critical mediator of NF-kappaB-dependent osteoclast survival preventing TNFalpha-induced cell death, and is required for formation of fully functional bone-resorbing osteoclasts and for inflammation-induced bone loss
-
-
?
additional information
?
-
-
IKK is required for activation of NF-kappaB and subsequent signalling pathways
-
-
?
additional information
?
-
-
IKK is responsible for NF-kappaB activation by inactivating its inhibitor IkappaB, different inflammation stimuli induce distinct IKK activity profiles, molecular mechanism, overview
-
-
?
additional information
?
-
-
IKKalpha, not IKKbeta, is required for epidermal regeneration, IkappaB kinases are essential key regulators of the canonical and noncanonical NFkappaB pathways important for the expression of a wide variety of genes that are involved in the control of immune and inflammatory response, and in the regulation of cellular proliferation and survival, mechanism, overview
-
-
?
additional information
?
-
-
IKKbeta is required for activation of NFkappaB, IKKbeta induces expression of epithelial sodium channel alphabetagamma-ENaC in cell surfaces
-
-
?
additional information
?
-
-
IKKbeta is required for regulation of NFkappaB activity and peripheral B cell survival and proliferation
-
-
?
additional information
?
-
-
parasite Toxoplasma gondii IKKalpha, localized in parasitophorous vacuole membrane, activates the host intracellular NF-kappaB in early infection stage resulting in NF-kappaB nuclear translocation and subsequent gene expression independently from the host IKK complex
-
-
?
additional information
?
-
-
subunit IKKbeta controls the activation of NF-kappaB, important in inflammation, IKKalpha plays a role in lyphoid organogenesis and suppresses NF-kappaB activity by accelerating both the turnover of the NFkappaB subunits RelA and c-Rel, and their removal from pro-inflammatory gene promoters, inactivation of IKKalpha enhances inflammation and bacterial clearance in mice, overview
-
-
?
additional information
?
-
-
activated IKK2 is responsible for induction of leucocyte infiltration in pancreatic acini, the mutant ICC2CA in pancreatic acinar cells increases tissue damage of secretagogue induced experimental pancreatitits, the enzyme is involved in the proinflammatory IKK/NF-kappaB pathway, overview
-
-
?
additional information
?
-
-
IkappaB kinase beta plays a critical role in metallothionein-1 expression and protection against arsenic toxicity, two signaling pathways appear to be important for modulating arsenic toxicity. First, the IKK-NF-kappaB pathway is crucial for maintaining cellular metallothionein-1 levels to counteract reactive oxygen species accumulation, and second, when this pathway fails, excessive reactive oxygen species leads to activation of the MKK4-JNK pathway, resulting in apoptosis
-
-
?
additional information
?
-
-
IkappaB kinase beta plays an essential role in remodeling Carma1-Bcl10-Malt1 complexes upon T cell activation, T cell receptor signaling to IkappaB kinase/NF-kappaB is controlled by PKCtheta-dependent activation of the Carma1, Bcl10, and Malt1 CBM complex, IKKbeta triggers the CBM complex formation and phosphorylation of Bcl by PMA/ionomycin or CD3/CD28, regulation, overview
-
-
?
additional information
?
-
-
IkappaB kinase-alpha is critical for interferon-alpha production induced by Toll-like receptors 7 and 9, but IKK-a is dispensable for a cytoplasmic RNA helicase RIG-I-dependent cytosolic pathway-induced production of IFN-alpha in MEF cells, overview
-
-
?
additional information
?
-
-
IKK-related kinases tank-binding kinase 1 TBK1/IKKi and cullin-based ubiquitin ligases are involved in IFN regulatory factor-3, IRF-3, phosphorylation, activation, and degradation, IRF-3 activation is induced by viral infection, e.g. by HCMV, molecular mechanisms, detailed overview
-
-
?
additional information
?
-
-
IKKalpha and IKKbeta are distinctly involved in ERK1-dependent, but IkappaBalpha-P65- and p100-p52-independent, upregulation of MUC5AC mucin transcription in case of infection by Streptococcus pneumoniae, MUC5AC mucin induction also requires pneumolysin and TLR4-dependent MyD88-IRAK1-TRAF6 signaling, molecular mechanism, overview
-
-
?
additional information
?
-
-
IKKalpha enhances p73-mediated transactivation and pro-apoptotic functions in p53-deficient H1299 cells, stabilization of p73, but not of the antagonist p53, by nuclear IKKalpha mediates cisplatin-induced apoptosis, DNA damage-induced accumulation of both p53 and p73alpha is associated with the up-regulation of IKK-alpha and IKK-gamma, a functional interaction might exist between them in DNA damage-mediated apoptotic pathways
-
-
?
additional information
?
-
-
IKKalpha is involved in the noncanonical NF-kappaB activation pathway, and plays an essential role in thymic organogenesis required for the establishment of self-tolerance, overview
-
-
?
additional information
?
-
-
IKKalpha is not only a regulator of mammary epithelial proliferation, but is also an important contributor to ErbB2-induced oncogenesis, providing signals that maintain mammary tumor-initiating cells, IKKalpha activity is required for cyclin D1 induction and proliferation of lobuloalveolar epithelial cells, and is required for self-renewal of ErbB2/Her2-transformed mammary tumor-initiating cells, overview
-
-
?
additional information
?
-
-
IKKepsilon is important in the regulation of the alternative NF-kappaB activation pathway involving p52 and p65, IKKepsilon interacts with p52 and promotes transactivation via p65
-
-
?
additional information
?
-
-
IKKepsilon, i.e. IKKi, is implicated in virus induction of interferon-beta, IFNbeta, and development of immunity, IKKepsilon functions in a redundant role to its ubiquitous counterpart, TBK1, in the activation of IRF3 and IRF7 ex vivo, IKKe determines ISGF3 binding specificity, regulaiton, overview
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additional information
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mechanisms/pathways of activation and derepression of the IKK complex, regulation, detailed overview
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additional information
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IKKalpha and IKKbeta are distinctly involved in ERK1-dependent, but IkappaBalpha-P65- and p100-p52-independent, upregulation of MUC5AC mucin transcription in case of infection by Streptococcus pneumoniae, MUC5AC mucin induction also requires pneumolysin and TLR4-dependent MyD88-IRAK1-TRAF6 signaling, molecular mechanism, overview
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additional information
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activation of NFkappaB by the catalytic subunit IKKbeta is required for signaling via the NFkappaB pathway in acute and systemic inflammation and for tissue protection
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additional information
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the IkappaB kinase regulates chromatin structure during reconsolidation of conditioned fear memories, IKKalpha is involved in the regulation of histone H3 phosphorylation and acetylation at specific gene promoters in hippocampus in the NF-kappaB pathway, inhibition of IKKalpha regulation results in impairments in fear memory reconsolidation, mechanism, overview
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(1R,4R)-4-(2-amino-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-cyclohexanol
-
(4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)phenyl)acetic acid
-
IC50 for the IKKbeta is 0.0022 mM
(E)-2-methoxy-4-(3-(4-methoxyphenyl)prop-1-en-1-yl)phenol
the compound directly binds to the ATP binding site of the enzyme with a strong binding affinity
-
(E)-4-[3-(5-(adamant-1-yl)-2-(but-1-oxy)-4-(2-methoxyethoxymethoxy)-phenyl)-3-oxoprop-1-en-1-yl]benzoic acid
shows highest inhibition of IKKbeta and highest induction of apoptosis in Jurkat cells
(E)-4-[3-(5-(adamant-1-yl)-2-(hexyl-1-oxy)-4-(2-methoxyethoxymethoxy)phenyl)-3-oxoprop-1-en-1-yl]benzoic acid
exhibits improved anti-IKKbeta and growth inhibitory activities and has lost its RAR-dependent transactivation function
(E)-4-[3-(5-(adamant-1-yl)-2-ethoxy-4-(2-methoxyethoxymethoxy)phenyl)-3-oxoprop-1-en-1-yl]benzoic acid
-
(E)-4-[3-(5-(adamant-1-yl)-4-(2-methoxyethoxymethoxy)-2-(pentyl-1-oxy)phenyl)-3-oxoprop-1-en-1-yl]benzoic acid
-
(E)-4-[3-(5-(adamant-1-yl)-4-(2-methoxyethoxymethoxy)-2-(prop-2-en-1-oxy)phenyl)-3-oxoprop-1-en-1-yl]benzoic acid
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(E)-4-[3-(5-(adamant-1-yl)-4-(2-methoxyethoxymethoxy)-2-(prop-2-yn-1-oxy)phenyl)-3-oxoprop-1-en-1-yl]benzoic acid
shows highest inhibition of IKKbeta and highest induction of apoptosis in Jurkat cells
(E)-4-[3-(5-(adamant-1-yl)-4-(2-methoxyethoxymethoxy)-2-phenylmethoxy-phenyl)-3-oxoprop-1-en-1-yl]benzoic acid
exhibits improved anti-IKKbeta and growth inhibitory activities and has lost its RAR-dependent transactivation function
(E)-4-[3-(5-adamant-1-yl-4-(2-methoxyethoxymethoxy)-2-(prop-1-oxy)-phenyl)-3-oxoprop-1-en-1-yl]benzoic acid
-
(R)-2-amino-4-(2-(hydroximethyl)pyrrolidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
(R)-2-amino-4-(3-hydroxypyrrolidin-1-yl)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
-
(S)-2-amino-4-(2-(hydroximethyl)pyrrolidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
1-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-sulfonamide
-
1-(4-chlorophenyl)-4-ureido-1H-pyrazole-3-carboxamide
i.e. SC-108
1-(6-chloro-9H-beta-carbolin-8-yl)-3-methylurea
-
inhibits IKK with IC50 of 0.02 mM
1-(benzo[d][1,3]dioxol-5-yl)-8-(3-chloroisonicotinamido)-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide
i.e. PHA-379
1-(benzo[d][1,3]dioxol-5-yl)-8-(5-chloro-2-(4-methylpiperazin-1-yl)isonicotinamido)-4,5-dihydro-1H-benzo-[g]indazole-3-carboxamide
i.e. PHA-250
1-[(3,4,5-trimethoxyphenyl)methyl]-1,2,3,4-tetrahydroisoquinoline-6,7-diol
NCI0288748, 65% inhibition at 0.1 mM
1-[3-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanamine
-
-
1-[4-(1-hydroxynaphthalen-2-yl)-6-imino-3-methyl-6,7-dihydropyrazolo[3,4-d][1,3]thiazin-1(4H)-yl]-2-phenylethan-1-one
NCI0657381, 76% inhibition at 0.1 mM
1-[4-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanamine
-
-
1-[4-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanesulfonamide
-
-
15d-prostaglandin J2
-
strongly inhibits IKK
17-acetoxyjolkinolide B
17-AJB is isolated from a traditional Chinese medicinal herb Euphorbia fischeriana Steud. 17-AJB interacts with IKK directly and keeps IKK in its phosphorylated form irreversibly, inactivating its kinase activity, leading to its failure to activate NF-kappaB. The effect of 17-AJB on IKK is specific. It has no effect on other kinases such as p38, p44/42, and JNK. 17-AJB induces apoptosis in tumor cells
2,4-diamino-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
2-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-benzenesulfonamide
-
2-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)benzamide
-
2-(4-fluorophenyl)-8-methyl-N-[2-(piperidin-1-yl)ethyl]-8H-imidazo[4,5-d][1,3]thiazolo[5,4-b]pyridin-5-amine
-
-
2-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzoic acid
-
IC50 for the IKK complex is above 0.1 mM
2-amino-4-((1R,2S,3R,4S)-2,3,4-trihydroxycyclopentylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
2-amino-4-((1R,4R)-4-hydroxycyclohexylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
2-amino-4-((1R,4R)-4-hydroxycyclohexylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carboxamide
-
2-amino-4-((1RS,2SR,3RS)-2,3-dihydroxycyclopentylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
2-amino-4-((cyclopropylmethyl)amino)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
-
2-amino-4-(2-(hydroxymethyl)phenyl)-7H-pyrrolo[2,3-d]- pyrimidine-5-carbonitrile
-
2-amino-4-(2-fluorophenyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
2-amino-4-(2-hydroxyethylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
2-amino-4-(2-hydroxyphenyl)-77H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
2-amino-4-(2-morpholinoethylamino)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
-
2-amino-4-(3-(hydroxymethyl)phenyl)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
-
2-amino-4-(3-fluorophenyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
2-amino-4-(3-hydroxypropylamino)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
-
2-amino-4-(3-hydroyphenyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
2-amino-4-(4-(2-hydroxyethyl)piperazin-1-yl)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
-
2-amino-4-(4-(methylsulfonyl)phenyl)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
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2-amino-4-(4-fluorophenyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
2-amino-4-(4-hydroxymethyl)phenyl-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
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2-amino-4-(4-hydroxyphenyl)-7H-pyrrolo[2,3-d]pyrimdine-5-carbonitrile
-
2-amino-4-(4-methylpiperazin-1-yl)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
-
2-amino-4-(4-phenylpiperazin-1-yl)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
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2-amino-4-(benzylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
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2-amino-4-(cyclohexyl(2-hydroxyethyl)amino)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
-
2-amino-4-(cyclohexylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
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2-amino-4-(cyclohexylmethylamino)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
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2-amino-4-(methylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
2-amino-4-(phenylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
2-amino-4-(piperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
2-amino-4-chloro-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
2-amino-4-morpholino-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
2-amino-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
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2-amino-6-(2-hydroxy-6-isobutoxyphenyl)-4-(piperidin-3-yl)nicotinonitrile
i.e. PHA-535E
2-benzamido-pyrimidines
-
diverse derivatives, synthesis and inhibitory potential determination, overview
2-hydroxy-N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]acetamide
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2-methanesulfonyl-4-methyl-7-methylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
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2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7yl)pyridin-2-yl)methyl)acetamide
2-[[bis(2-hydroxyethyl)amino]methyl]-4-(2-methylbutan-2-yl)phenol
NCI0079692, 59% inhibition at 0.1 mM
3-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimdin-4-yl)benzamide
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3-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-benzenesulfonamide
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3-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzoic acid
-
IC50 for the IKKbeta is 0.001 mM
3-amino-4,6-dimethylthieno[2,3-b]pyridine-2-carboxamide
-
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3-amino-4-(1-benzofuran-2-yl)-6-methylthieno[2,3-b]pyridine-2-carboxamide
-
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3-amino-4-(2-methoxyethoxy)thieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-4-(4-chlorophenyl)-6-methylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-4-(4-hydroxyphenyl)-6-methylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-4-ethoxythieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-4-furan-2-yl-6-methylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-4-methoxythieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-4-methyl-6-morpholin-4-ylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-4-methyl-6-piperazin-1-ylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-4-methyl-6-piperidin-1-ylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-4-propoxythieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-(1,4-diazepan-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-(2-aminoethoxy)-4-methylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-(2-hydroxyethoxy)-4-methylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-(3-aminoazepan-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-(3-aminopropoxy)-4-methylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-(3-hydroxypiperidin-1-yl)-4-methylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-(3-hydroxypiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-(3-hydroxypropoxy)-4-methylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-(3-oxo-1,4-diazepan-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-(3-oxopiperazin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-(4-aminopiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-(4-carbamoylpiperazin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-(4-carbamoylpiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-(4-hydroxy-3,3-dimethylpiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-(4-hydroxypiperidin-1-yl)-4-methylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-(4-hydroxypiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-(4-methoxypiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-(4-methylpiperazin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-methyl-4-(2-methylpropyl)thieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-methyl-4-(4-methylphenyl)thieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-methyl-4-phenylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-methyl-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-methyl-4-pyridin-2-ylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-methyl-4-thiophen-2-ylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-methyl-4-[4-(methylsulfonyl)phenyl]thieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-methylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-piperazin-1-yl-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-[(2-hydroxyethyl)amino]-4-methylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-[(3R)-3-aminopyrrolidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-[(3R)-3-hydroxypyrrolidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-[(3S)-3-aminopyrrolidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-[(3S)-3-hydroxypyrrolidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
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3-amino-6-[4-(dimethylamino)piperidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-[4-(methylamino)piperidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-amino-6-[4-[(methylsulfonyl)amino]piperidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
-
-
3-methoxy-N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]propanamide
-
3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzonitrile
-
3-[7-(benzyloxy)isoquinolin-6-yl]benzenesulfonamide
-
-
3-[7-(piperidin-4-yloxy)isoquinolin-6-yl]benzenesulfonamide
-
-
4'-amino-4-chloro-4''-sulfamoyl-1,1':3',1''-terphenyl-5'-carboxamide
-
-
4,8-dimethoxy-1-vinyl-beta-carboline
-
i.e. beta-carboline alkaloid C-1, isolated from Melia azedarach var. japonica, inhibits IKK activity by reduction of IKK phosphorylation and degradation, and activation and nuclear translocation of NF-kappaB and subsequent signalling pathways
4-((2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-benzenesulfonamide
-
4-((2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-benzoic acid
-
4-(1-benzothiophen-2-yl)-N-[3-chloro-4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
-
IC50 for the IKK complex is 250 nM
4-(1-benzothiophen-2-yl)-N-[3-methoxy-4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
-
IC50 for the IKK complex is 150 nM
4-(1-benzothiophen-2-yl)-N-[4-(pyrrolidin-1-ylcarbonyl)phenyl]pyrimidin-2-amine
-
IC50 for the IKK complex is 0.0085 mM, cellular profile
4-(1-benzothiophen-2-yl)-N-[4-([4-(dimethyl-amino)piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
-
IC50 for the IKK complex is 80 nM, cellular profile
4-(1-benzothiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
-
IC50 for the IKK complex is 70 nM, cellular profile
4-(2'-aminoethyl)amino-1,8-dimethylimidazo(1,2-a)quinoxaline
4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimdin-4-yl)benzamide
-
4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-benzenesulfonamide
-
4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-N-(p-tolyl)-benzenesulfonamide
-
4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-N-methylbenzenesulfonamide
-
4-(2-amino-7H-pyrrol[2,3-d]pyrimidin-4-yl)benzenesulfonamide
-
4-(5-(3-acetamino-3-methylbutyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
-
IC50 for the IKK complex is 800 nM
4-(5-(3-amino-3-ethylpentyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
-
IC50 for the IKK complex is 30 nM
4-(5-(3-amino-3-methyl-but-1-ynyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
-
IC50 for the IKK complex is 200 nM
4-(5-(3-amino-3-methyl-butyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
-
IC50 for the IKK complex is 40 nM
4-(5-(3-hydroxy-3-methylbutyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amin
-
IC50 for the IKK complex is 50 nM, cellular profile
4-(5-(3-methoxypropyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
-
IC50 for the IKK complex is 100 nM, cellular profile
4-(5-(4-hydroxybutyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
-
IC50 for the IKK complex is 40 nM, cellular profile
4-(5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)benzenesulfonamide
-
4-(7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]isoquinolin-6-yl)benzenesulfonamide
-
-
4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)benzenesulfonamide
-
4-(piperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidin-2-amine
-
4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzoic acid
-
IC50 for the IKK complex is 0.018 mM, cellular profile
4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-amine
-
4-methyl-7-methylamino-2-(azepan-1-yl)-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
-
4-methyl-7-methylamino-2-(methylthio)-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
-
4-methyl-7-methylamino-2-benzylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
-
4-methyl-7-methylamino-2-cyclopentylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
-
4-methyl-7-methylamino-2-diethylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
-
4-methyl-7-methylamino-2-ethylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
-
4-methyl-7-methylamino-2-hydroxyethylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
-
4-methyl-7-methylamino-2-methylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
-
4-methyl-7-methylamino-2-methylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
-
4-methyl-7-methylamino-2-piperidine-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
-
4-methyl-7-methylamino-2-thienylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
-
4-methyl-7-methylamino-2-[1,2,3,6-tetrahydropyridine]-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
-
4-[6-[(2-hydroxyethyl)amino]-7-methyl-7,8-dihydro-2H,6H-[1,3]dioxolo[4,5-g][1]benzopyran-8-yl]-2,6-dimethoxyphenol
NCI0671177, 68% inhibition at 0.1 mM
4-[7-(benzyloxy)isoquinolin-6-yl]benzenesulfonamide
-
-
4-[7-(piperidin-3-ylmethoxy)isoquinolin-6-yl]benzenesulfonamide
-
-
4-[7-(piperidin-3-yloxy)isoquinolin-6-yl]benzenesulfonamide
-
-
4-[7-(piperidin-4-ylmethoxy)isoquinolin-6-yl]benzenesulfonamide
-
-
4-[7-(piperidin-4-yloxy)isoquinolin-6-yl]benzenesulfonamide
-
-
4-[7-[(1-acetylpiperidin-4-yl)oxy]isoquinolin-6-yl]benzenesulfonamide
-
-
4-[N'-(4,6-dimethylpyrimidin-2-yl)carbamimidamido]-N-(phenylcarbamoyl)benzene-1-sulfonamide
NCI0107328, 94% inhibition at 0.1 mM
5,6-dibromo-beta-carboline
-
inhibits IKK with IC50 of 600 nM
5-((3-fluorophenyl)ethynyl)-2-ureidothiophene-3-carboxamide
i.e. PHA-966
5-(4-fluorophenyl)-2-ureidothiophene-3-carboxamide
i.e. SC-440
5-amino-2,30-bithiophene-4-carboxamide
i.e. SC-514
5-Aminosalicylate
-
weak inhibition of IKK-2
5-bromo-6-chloro-beta-carboline
-
inhibits IKK with IC50 of 600 nM
5-bromo-6-cyano-beta-carboline
-
inhibits IKK with IC50 of 0.0011 mM
5-bromo-6-fluoro-beta-carboline
-
inhibits IKK with IC50 of 0.002 mM
5-bromo-6-methoxy-beta-carboline
-
nonspecific inhibitor of IKK, inhibits IKK with IC50 of 0.004 mM
5-bromo-6-trifluoromethyl-beta-carboline
-
inhibits IKK with IC50 of 0.0011 mM
5-bromo-beta-carboline
-
inhibits IKK with IC50 of 0.015 mM
6,6-dimethyl-1-[3-[3-(3-nitrophenoxy)propoxy]phenyl]-1,3,5-triazinane-2,4-diimine
NCI0111727, 75% inhibition at 0.1 mM
6,8-dichloro-7-(cyclohexylmethoxy)-9H-beta-carboline
-
inhibits IKK with IC50 of 0.003 mM
6,8-dichloro-7-ethoxy-9H-beta-carboline
-
inhibits IKK with IC50 of 140 nM
6,8-dichloro-7-methoxy-9H-beta-carboline
-
inhibits IKK with IC50 of 170 nM
6,8-dichloro-9H-beta-carbolin-7-yl morpholine-4-carboxylate
-
inhibits IKK with IC50 of 0.0032 mM
6,8-dichloro-beta-carboline
-
inhibits IKK with IC50 of 200 nM
6-bromo-7-(piperidin-4-yloxy)isoquinoline
-
-
6-bromo-7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]isoquinoline
-
-
6-phenyl-7-(piperidin-3-ylmethoxy)isoquinoline
-
-
6-phenyl-7-(piperidin-3-yloxy)isoquinoline
-
-
6-phenyl-7-(piperidin-4-ylmethoxy)isoquinoline
-
-
6-phenyl-7-(piperidin-4-yloxy)isoquinoline
-
-
6-phenyl-7-(pyridin-3-ylmethoxy)isoquinoline
-
-
6-phenyl-7-(pyridin-4-ylmethoxy)isoquinoline
-
-
7-(2-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
-
7-(3-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
-
7-(3-methoxyphenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
-
7-(3-[[2-(3,5-dihydroxyphenyl)-2-hydroxyethyl]amino]propyl)-1,3-dimethyl-8-(morpholin-4-yl)-3,7-dihydro-1H-purine-2,6-dione
NCI0293897, 55% inhibition at 0.1 mM
7-(4-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
-
7-(OCH2CH(CH2CH2))-6,8-dichloro-beta-carboline
-
inhibits IKK with IC50 of 80 nM
7-(piperidin-4-yloxy)isoquinoline
-
-
7-hydroxy-6,8-dichloro-beta-carboline
-
inhibits IKK with IC50 of 0.011 mM
7-[(1-acetylpiperidin-4-yl)oxy]-6-bromoisoquinoline
-
-
7-[(1-acetylpiperidin-4-yl)oxy]-6-phenylisoquinoline
-
-
7-[3-(aminomethyl)phenyl]-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
-
7-[[1-(ethylsulfonyl)piperidin-4-yl]methoxy]-6-phenylisoquinoline
-
-
7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]-6-phenylisoquinoline
-
-
8-(5-chloro-2-(4-methylpiperazin-1-yl)isonicotinamido)-1-(4-fluorophenyl)-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide
8-amino-6-chloro-beta-carboline
-
inhibits IKK with IC50 of 0.0013 mM
8-dimethylamino-6-chloro-beta-carboline
-
inhibits IKK with IC50 of 0.0018 mM
8-methyl-2-(4-fluorophenyl)-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine
-
-
8-methylamino-6-chloro-beta-carboline
-
inhibits IKK with IC50 of 0.0018 mM
8-nitro-6-chloro-beta-carboline
-
inhibits IKK with IC50 of 0.004 mM
acetamide,N-[2-[[2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-yl]amino]ethyl]
-
-
Acetylsalicylate
-
weak inhibition of IKK-2
antirheumatic gold compound
-
inhibition of IKKbeta
-
arsenite
-
inhibition of IKKbeta
Berberine
an isoquinoline alkaloid derived from a plant used traditionally in Chinese and Ayurvedic medicine inhibits IKK activity. Addition of DTT to the kinase reaction reverses the berberine-mediated inhibition of IKK activity
BI605906
-
an IKKbeta inhibitor
BMS-345541
-
specific for IKK-2, binds at an allosteric site
BMS345541
shows efficacy in a mouse model of collagen-induced arthritis without signs of major toxicology
chrysin
chrysin interacts weakly with the I-kappa-B kinase epsilon binding site and inhibits the enzyme at doses higher than 0.06 mM
COMPOUND A
leads to a significant reduction of Panc-1 cell and MiaPaCa-2 cell growth
curcumin
-
weak inhibition of IKK-2
cyclopentenone prostaglandins
cyclopentenone prostanoids
-
inhibition of IKK and thus inhibition of NFkappaB-mediated HSV-1-induced HIV-1 replication
cyclopentone prostaglandines
-
inhibition of IKK-2
ethanol,N-[2-[[2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-yl]amino]ethyl]
-
-
evodiamine
-
alkaloid extracted from Evodia rutaecarpa fruits exhibiting antiproliferative, antimetastatic, and apoptotic activities, inhibits IKKalpha activity, suppresses IKKalpha phosphorylation and degradation, and specifically blocks NF-kappaB activation by IKK and other agents, translocation, and activity, overview
LY294002
phosphorylation of IKKalphaT23 is inhibited both by LY294002 and wortmannin, but phosphorylation of Ser176/Ser180 is not
lysyl-N-(4-methoxynaphthalen-2-yl)alaninamide
NCI0339925, 93% inhibition at 0.1 mM
methyl (6-chloro-9H-beta-carbolin-8-yl)carbamate
-
inhibits IKK with IC50 of 700 nM
methyl 1-(3-amino-2-carbamoyl-4-propylthieno[2,3-b]pyridin-6-yl)piperidine-4-carboxylate
-
-
MRT67307
-
an IKKepsilon/TBK1 kinase inhibitor
MX781
0.02 mM inhibit IKKbeta by 65% in the presence of an ATP concentration corresponding to its Km value
N,1-dimethyl-7-phenyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
-
N,1-dimethyl-7-phenyl-1H-pyrazolo[5,1-b]purin-4-amine
-
-
N,3,8-trimethyl-2-phenyl-3,8-dihydrodiimidazo[4,5-b:4',5'-d]pyridin-5-amine
-
N,8-dimethyl-2-phenyl-8H-imidazo[4,5-d][1,3]oxazolo[5,4-b]pyridin-5-amine
-
N,8-dimethyl-2-phenyl-8H-imidazo[4,5-d][1,3]thiazolo[5,4-b]pyridin-5-amine
-
N,N-dimethyl-3-[(4-[[(6-phenylisoquinolin-7-yl)oxy]methyl]piperidin-1-yl)sulfonyl]propan-1-amine
-
-
N-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)ethane-1,2-diamine
-
-
N-(2-aminoethyl)-4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzamide
-
IC50 for the IKK complex is 0.0044 mM
N-(2-dimethyl-aminoethyl)-4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzamide
-
IC50 for the IKK complex is 300 nM, cellular profile
N-(2-pyrrolidin-1-yl-ethyl)-4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzamide
-
IC50 for the IKK complex is 500 nM
N-(3,5-bis-trifluoromethylphenyl)-5-chloro-2-hydroxybenzamide
-
-
N-(3-methyl-butyl)-4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzamide
-
IC50 for the IKKbeta is above 0.1 mM
N-(3-[2-imino-6-methyl-3-[(3-nitrophenyl)methyl]-4-oxo-1,2,3,4-tetrahydropyrimidin-5-yl]propyl)-4-methylbenzene-1-sulfonamide
NCI0211135, complete inhibition at 0.1 mM
N-(4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)-methanesulfonamide
-
N-(6-chloro-9H-beta-carbolin-8-yl)-2-(pyridin-2-yl)acetamide
-
inhibits IKK with IC50 of 0.003 mM
N-(6-chloro-9H-beta-carbolin-8-yl)-2-methoxybenzamide
-
inhibits IKK with IC50 of 0.02 mM
N-(6-chloro-9H-beta-carbolin-8-yl)-3-methoxybenzamide
-
inhibits IKK with IC50 of 600 nM
N-(6-chloro-9H-beta-carbolin-8-yl)-4-hydroxybutanamide
-
inhibits IKK with IC50 of 0.02 mM
N-(6-chloro-9H-beta-carbolin-8-yl)-4-methoxybenzamide
-
inhibits IKK with IC50 of 0.0013 mM
N-(6-chloro-9H-beta-carbolin-8-yl)acetamide
-
inhibits IKK with IC50 of 600 nM
N-(6-chloro-9H-beta-carbolin-8-yl)benzamide
-
inhibits IKK with IC50 of 700 nM
N-(6-chloro-9H-beta-carbolin-8-yl)benzenesulfonamide
-
inhibits IKK with IC50 of 0.02 mM
N-(6-chloro-9H-beta-carbolin-8-yl)methanesulfonamide
-
inhibits IKK with IC50 of 0.0083 mM
N-(6-chloro-9H-beta-carbolin-8-yl)morpholine-4-carboxamide
-
inhibits IKK with IC50 of 0.02 mM
N-(6-chloro-9H-beta-carbolin-8-yl)pyridine-2-carboxamide
-
inhibits IKK with IC50 of 0.001 mM
N-(6-chloro-9H-beta-carbolin-8-yl)pyridine-4-carboxamide
-
inhibits IKK with IC50 of 300 nM
N-(8-methyl-2-phenylimidazo[1,2-a]thieno[3,2-e]pyrazin-5-yl)ethane-1,2-diamine
-
-
N-acetylcysteine
inhibits phosphorylation of IkappaBalpha
N-benzyl-6-chloro-9H-beta-carbolin-8-amine
-
inhibits IKK with IC50 of 0.02 mM
N-ethyl-2-(4-fluorophenyl)-N-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine
-
-
N-methyl-2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine
-
-
N-tosyl-L-phenylalanine chloromethyl ketone
-
-
N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]-1,2,3-thiadiazole-4-carboxamide
-
N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]acetamide
-
N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]butanediamide
-
N-[5-[4-(cyclopropylamino)-1-methyl-1H-pyrazolo[5,1-b]purin-7-yl]-2-fluorobenzyl]acetamide
-
-
N-[[2-fluoro-5-[8-methyl-5-methylamino-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]acetamide
-
-
N-[[2-fluoro-5-[8-methyl-5-methylamino-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]methanesulfonamide
-
-
N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]-1,2,3-thiadiazole-5-amide
-
-
N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]acetamide
-
-
N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]isoxazole-5-amide
-
-
N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]methanesulfonamide
-
-
N1-(1,8-dimethylimidazo-[1,2-a]quinoxalin-4-yl)ethane-1,2-diamine
i.e. PHA-068E
N2,N2-dimethyl-N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]glycinamide
-
N2-(2-chlorophenyl)-N-[6-[(2-chlorophenyl)sulfamoyl]-2-methyl-4-oxoquinazolin-3(4H)-yl]glycinamide
NCI0687760, 89% inhibition at 0.1 mM
N4-cyclohexyl-5-(trifluoromethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
-
N4-cyclohexyl-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
-
NBD peptide
-
NEMO-binding domain peptide
-
nimbolide
-
nimbolide inhibits TNF-alpha-induced p65 nuclear translocation and phosphorylation. Nimbolide binds to and inhibits IKK activation. It suppresses NF-betaB activation by inhibition of IkappaBbeta kinase, wild-type not IKKbeta mutant C179A, leading to suppression of IkappaBalpha phosphorylation and degradation, nuclear translocation, DNA binding, and gene transcription
prostaglandin 2alpha
-
inhibits IKK
prostaglandin A1
-
strongly inhibits IKK
Prostaglandin A2
-
strongly inhibits IKK
prostaglandin E1
-
inhibits IKK
prostaglandin E2
-
inhibits IKK
protein HSCARG
-
or NMRAL1, NmrA-like family domain-containing protein 1, inhibits the phosphorylation of IKKbeta
-
PS-1145
-
i.e. 8-(NHC(O)-3'-pyridyl)-6-chloro-beta-carboline, inhibits IKK with IC50 of 100 nM in vitro, blocks phosphorylation of IkappaBalpha and subsequent activation of NFkappaB in vivo
PS1145
-
inhibits IKK, blocks TNFalpha activation by IKK in vivo
Rapamycin
suppresses IKK activity potentailly through dissociation of raptor from the mTOR complex; suppresses IKK activity potentailly through dissociation of raptor from the mTOR complex
ring finger protein 8
-
upon TNFalpha stimulation, ring finger protein 8 binds to the catalytic subunits of the enzyme complex, resulting in inhibition of IkappaB kinase alpha/beta phosphorylation and subsequent nuclear factor-kappaB activation
-
salicylate
-
weak inhibition of IKK-2
SC-514
i.e. 4-amino-[2,3'-bithiophene]-5-carboxamide
-
tetrandrine
-
a bis-benzylisoquinoline alkaloid isolated from the roots of Han-Fang-Ji (Stephania Tetrandra S Moore) effectively inhibits IKKs phosphorylation
vaccina virus virulence factor B14
-
interacts and inhibits IKKcomplex. Interaction between vaccina virus virulence factor B14 and IKK complex requires IKKbeta but not IKKalpha
-
vaccinia virus virulence factor B14
-
interacts and inhibits IKKcomplex. Interaction between B14 and IKK complex requires IKKbeta but not IKKalpha
-
Wortmannin
phosphorylation of IKKalphaT23 is inhibited both by LY294002 and wortmannin, but phosphorylation of Ser176/Ser180 is not
YopJ
-
effector protein YopJ from Yersinia pestis inhibits MAPK kinase and IKK activation by acetylating the conserved serine and threonine residues in the activation loop of the kinase. Furthermore, YopJ inhibits Tax-mediated IkappaB phosphorylation
-
2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7yl)pyridin-2-yl)methyl)acetamide
-
BMS-066, inhibitor of IKKbeta
2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7yl)pyridin-2-yl)methyl)acetamide
-
BMS-066, inhibitor of IKKbeta
2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7yl)pyridin-2-yl)methyl)acetamide
-
BMS-066, inhibitor of IKKbeta
2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7yl)pyridin-2-yl)methyl)acetamide
-
BMS-066, inhibitor of IKKbeta
4-(2'-aminoethyl)amino-1,8-dimethylimidazo(1,2-a)quinoxaline
-
BMS-345541, inhibitor of IKKbeta
4-(2'-aminoethyl)amino-1,8-dimethylimidazo(1,2-a)quinoxaline
-
BMS-345541, inhibitor of IKKbeta
4-(2'-aminoethyl)amino-1,8-dimethylimidazo(1,2-a)quinoxaline
-
BMS-345541, inhibitor of IKKbeta
4-(2'-aminoethyl)amino-1,8-dimethylimidazo(1,2-a)quinoxaline
-
BMS-345541, inhibitor of IKKbeta
8-(5-chloro-2-(4-methylpiperazin-1-yl)isonicotinamido)-1-(4-fluorophenyl)-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide
PHA-408, ATP-competitive, selective IKK-2 inhibitor; PHA-408, ATP-competitive, selective IKK-2 inhibitor
8-(5-chloro-2-(4-methylpiperazin-1-yl)isonicotinamido)-1-(4-fluorophenyl)-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide
-
PHA-408, ATP-competitive, selective IKK-2 inhibitor
Acetylsalicylic acid
-
nonspecific for IKK, anti-inflammatory
Acetylsalicylic acid
-
nonspecific for IKK, anti-inflammatory
arsenic trioxide
-
nonspecific for IKK, acts on a cystein ersidue in the activation loop
arsenic trioxide
-
nonspecific for IKK, acts on a cystein ersidue in the activation loop
AS602868
-
IKKbeta inhibitor
AS602868
-
inhibitor of IKK-beta
AS602868
-
IKKbeta inhibitor
cyclopentenone prostaglandins
-
nonspecific for IKK, anti-inflammatory
cyclopentenone prostaglandins
-
inhibition of IKKbeta
cyclopentenone prostaglandins
-
nonspecific for IKK, anti-inflammatory
IMD-0354
-
specific IKKbeta inhibition
IMD-0354
-
in macrophages, the inhibition of IkappaB kinase beta (IKKbeta) results in lower proinflammatory cytokine expression caused by heat-killed Helicobacter pylori cells. Treatment with IKKbeta inhibitor results in milder inflammation in gerbils with Helicobacter pylori gastritis
IMD-0354
-
specific IKKbeta inhibition
PHA-408
a selective IKK-2 inhibitor, shows time-dependent binding to the enzyme
PHA-408
-
selective IKK-2 inhibitor
RNAi
-
specific IKKbeta inhibition
-
RNAi
-
specific IKKbeta inhibition
-
S1627
-
specific for the IKK complex, inhibits purified IKK in vitro with IC50 of 0.02 mM, inhibits IKK and NFkappaB nuclear translocation in vivo in umbilical vein endothelial cells and in rats, overview
-
S1627
preferentially inhibits the beta-subunit of the IKK complex. Specific inhibition of I-kappaB kinase by S1627 modulates the nociceptive response in various nociceptive models in rats. S1627 inhibits the activation of NF-kappaB in the spinal cord and thereby thermal and mechanical hyperalgesia in the zymosan-induced paw inflammation model and the inflammatory edema. It also reduces tactile and cold allodynia in a model of neuropathic pain
-
sulfasalazine
-
weak inhibition of IKK-2
sulfasalazine
-
nonspecific for IKK, anti-inflammatory
sulfasalazine
-
nonspecific for IKK, anti-inflammatory
sulindac sulfide
-
nonspecific for IKK, anti-inflammatory
sulindac sulfide
-
nonspecific for IKK, anti-inflammatory
TPCA-1
-
-
TPCA-1
i.e. 5-[(4-fluorophenyl)-2-ureido]thiophene-3-carboxamide
-
trans-resveratrol
-
nonspecific for IKK, anti-inflammatory
trans-resveratrol
-
nonspecific for IKK, anti-inflammatory
additional information
-
CREB-binding protein-bound NEMO/IKKgamma inhibits IKKalpha and p65 transcriptional activities
-
additional information
-
evodiamine analogue rutaecarpine does not inhibit IKK and NF-kappaB activation
-
additional information
-
simvastatin inhibits the TNFalpha-induced activation of IkappaB kinase and activation of NF-kappaB in vitro and in vivo, simvastatin highly affects the whole NF-kappaB-dependent pathway of signaling, overview
-
additional information
-
prolyl hydroxylase-1 negatively regulates IKKbeta, hydroxylation represses IKKbeta activity by altering protein expression or by preventing its activation through phosphorylation on S177/S181
-
additional information
structure-based design of IKK-2 inhibitors based on induced-fit docking into the homology model, overview
-
additional information
-
two structurally unrelated kinase inhibitors, termed NG25 or 5Z-7-oxozeaenol, inhibit the TAK1 protein kinase, and therefore also inhibit activation of IKKalpha and IKKbeta
-
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0.03
(1R,4R)-4-(2-amino-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-cyclohexanol
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.0022
(4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)phenyl)acetic acid
Homo sapiens
-
IC50 for the IKKbeta is 0.0022 mM
0.0025 - 0.03
(R)-2-amino-4-(2-(hydroximethyl)pyrrolidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
0.006 - 0.03
(R)-2-amino-4-(3-hydroxypyrrolidin-1-yl)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
0.0031 - 0.03
(S)-2-amino-4-(2-(hydroximethyl)pyrrolidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
0.00052 - 0.0043
1,4-dimethyl-7-methylamino-2-phenyl-4H-imidazo[4,5-d]imidazo[5,4-b]pyridine
0.0053 - 0.0059
1-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-sulfonamide
0.02
1-(6-chloro-9H-beta-carbolin-8-yl)-3-methylurea
Homo sapiens
-
inhibits IKK with IC50 of 0.02 mM
0.0008 - 0.0126
1-[3-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanamine
0.0001 - 0.0063
1-[4-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanamine
0.0004 - 0.004
1-[4-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanesulfonamide
0.0003
17-acetoxyjolkinolide B
Homo sapiens
-
0.03
2,4-diamino-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.03
2-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-benzenesulfonamide
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.03
2-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)benzamide
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.000056 - 0.0083
2-(4-fluorophenyl)-8-methyl-N-[2-(piperidin-1-yl)ethyl]-8H-imidazo[4,5-d][1,3]thiazolo[5,4-b]pyridin-5-amine
0.1
2-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzoic acid
Homo sapiens
-
IC50 for the IKK complex is above 0.1 mM
0.0008 - 0.0036
2-amino-4-((1R,2S,3R,4S)-2,3,4-trihydroxycyclopentylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
0.002 - 0.03
2-amino-4-((1R,4R)-4-hydroxycyclohexylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
0.03
2-amino-4-((1R,4R)-4-hydroxycyclohexylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carboxamide
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.001 - 0.03
2-amino-4-((1RS,2SR,3RS)-2,3-dihydroxycyclopentylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
0.016 - 0.03
2-amino-4-((cyclopropylmethyl)amino)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
0.03
2-amino-4-(2-(hydroxymethyl)phenyl)-7H-pyrrolo[2,3-d]- pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.002 - 0.03
2-amino-4-(2-fluorophenyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
0.0016 - 0.03
2-amino-4-(2-hydroxyethylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
0.015 - 0.03
2-amino-4-(2-hydroxyphenyl)-77H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
0.03
2-amino-4-(2-morpholinoethylamino)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.004 - 0.0098
2-amino-4-(3-(hydroxymethyl)phenyl)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
0.0077 - 0.03
2-amino-4-(3-fluorophenyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
0.0121 - 0.03
2-amino-4-(3-hydroxypropylamino)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
0.0024 - 0.0038
2-amino-4-(3-hydroyphenyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
0.03
2-amino-4-(4-(2-hydroxyethyl)piperazin-1-yl)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.0003 - 0.0024
2-amino-4-(4-(methylsulfonyl)phenyl)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
0.01 - 0.03
2-amino-4-(4-fluorophenyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
0.00065 - 0.0023
2-amino-4-(4-hydroxymethyl)phenyl-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
0.0016 - 0.02
2-amino-4-(4-hydroxyphenyl)-7H-pyrrolo[2,3-d]pyrimdine-5-carbonitrile
0.03
2-amino-4-(4-methylpiperazin-1-yl)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.03
2-amino-4-(4-phenylpiperazin-1-yl)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.0053 - 0.03
2-amino-4-(benzylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
0.03
2-amino-4-(cyclohexyl(2-hydroxyethyl)amino)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.0018 - 0.03
2-amino-4-(cyclohexylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
0.03
2-amino-4-(cyclohexylmethylamino)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.013 - 0.03
2-amino-4-(methylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
0.013 - 0.03
2-amino-4-(phenylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
0.0053 - 0.03
2-amino-4-(piperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
0.004 - 0.03
2-amino-4-chloro-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
0.02 - 0.03
2-amino-4-morpholino-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
0.0017 - 0.03
2-amino-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
0.000025
2-hydroxy-N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]acetamide
Homo sapiens
-
0.000081 - 0.0076
2-methanesulfonyl-4-methyl-7-methylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
0.000009 - 0.00496
2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7yl)pyridin-2-yl)methyl)acetamide
0.03
3-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimdin-4-yl)benzamide
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.0053 - 0.0059
3-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-benzenesulfonamide
0.001
3-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzoic acid
Homo sapiens
-
IC50 for the IKKbeta is 0.001 mM
0.0027
3-amino-4,6-dimethylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.0169
3-amino-4-(1-benzofuran-2-yl)-6-methylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.0108
3-amino-4-(2-methoxyethoxy)thieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.014
3-amino-4-(4-chlorophenyl)-6-methylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.02
3-amino-4-(4-hydroxyphenyl)-6-methylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta, larger than 0.0200
0.002
3-amino-4-ethoxythieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.0011
3-amino-4-furan-2-yl-6-methylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.0047
3-amino-4-methoxythieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.0025
3-amino-4-methyl-6-morpholin-4-ylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.00068
3-amino-4-methyl-6-piperazin-1-ylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.0024
3-amino-4-methyl-6-piperidin-1-ylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.0022
3-amino-4-propoxythieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.000072
3-amino-6-(1,4-diazepan-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.0029
3-amino-6-(2-aminoethoxy)-4-methylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.0066
3-amino-6-(2-hydroxyethoxy)-4-methylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.00063
3-amino-6-(3-aminoazepan-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.05
3-amino-6-(3-aminopropoxy)-4-methylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta, larger than 0.0500
0.0024
3-amino-6-(3-hydroxypiperidin-1-yl)-4-methylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.00057 - 0.0133
3-amino-6-(3-hydroxypiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
0.0051
3-amino-6-(3-hydroxypropoxy)-4-methylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.00014
3-amino-6-(3-oxo-1,4-diazepan-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.002
3-amino-6-(3-oxopiperazin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.000041 - 0.0016
3-amino-6-(4-aminopiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
0.00015
3-amino-6-(4-carbamoylpiperazin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.0013
3-amino-6-(4-carbamoylpiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.00075
3-amino-6-(4-hydroxypiperidin-1-yl)-4-methylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.00028 - 0.0112
3-amino-6-(4-hydroxypiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
0.00068
3-amino-6-(4-methoxypiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.00052
3-amino-6-(4-methylpiperazin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.0025
3-amino-6-methyl-4-(2-methylpropyl)thieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.0085
3-amino-6-methyl-4-(4-methylphenyl)thieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.0074
3-amino-6-methyl-4-phenylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.0013
3-amino-6-methyl-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.006
3-amino-6-methyl-4-pyridin-2-ylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.002
3-amino-6-methyl-4-thiophen-2-ylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.0013
3-amino-6-methyl-4-[4-(methylsulfonyl)phenyl]thieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.0127
3-amino-6-methylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.00012 - 0.0034
3-amino-6-piperazin-1-yl-4-propylthieno[2,3-b]pyridine-2-carboxamide
0.0058
3-amino-6-[(2-hydroxyethyl)amino]-4-methylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.0005
3-amino-6-[(3R)-3-aminopyrrolidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.00195
3-amino-6-[(3R)-3-hydroxypyrrolidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.00059
3-amino-6-[(3S)-3-aminopyrrolidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.00145
3-amino-6-[(3S)-3-hydroxypyrrolidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.00068
3-amino-6-[4-(dimethylamino)piperidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.00012
3-amino-6-[4-(methylamino)piperidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.000098
3-amino-6-[4-[(methylsulfonyl)amino]piperidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.000012 - 0.00262
3-methoxy-N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]propanamide
0.000007
3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzonitrile
Homo sapiens
-
0.0079 - 0.0251
3-[7-(benzyloxy)isoquinolin-6-yl]benzenesulfonamide
0.0013 - 0.0079
3-[7-(piperidin-4-yloxy)isoquinolin-6-yl]benzenesulfonamide
0.01 - 0.03
4-((2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-benzenesulfonamide
0.03
4-((2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-benzoic acid
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.00025
4-(1-benzothiophen-2-yl)-N-[3-chloro-4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
Homo sapiens
-
IC50 for the IKK complex is 250 nM
0.00015
4-(1-benzothiophen-2-yl)-N-[3-methoxy-4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
Homo sapiens
-
IC50 for the IKK complex is 150 nM
0.0085
4-(1-benzothiophen-2-yl)-N-[4-(pyrrolidin-1-ylcarbonyl)phenyl]pyrimidin-2-amine
Homo sapiens
-
IC50 for the IKK complex is 0.0085 mM, cellular profile
0.00008
4-(1-benzothiophen-2-yl)-N-[4-([4-(dimethyl-amino)piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
Homo sapiens
-
IC50 for the IKK complex is 80 nM, cellular profile
0.00007
4-(1-benzothiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
Homo sapiens
-
IC50 for the IKK complex is 70 nM, cellular profile
0.016 - 0.03
4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimdin-4-yl)benzamide
0.00008 - 0.001
4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-benzenesulfonamide
0.0014 - 0.016
4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-N-(p-tolyl)-benzenesulfonamide
0.0001 - 0.0014
4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-N-methylbenzenesulfonamide
0.00061 - 0.0029
4-(2-amino-7H-pyrrol[2,3-d]pyrimidin-4-yl)benzenesulfonamide
0.0008
4-(5-(3-acetamino-3-methylbutyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
Homo sapiens
-
IC50 for the IKK complex is 800 nM
0.00003
4-(5-(3-amino-3-ethylpentyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
Homo sapiens
-
IC50 for the IKK complex is 30 nM
0.0002
4-(5-(3-amino-3-methyl-but-1-ynyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
Homo sapiens
-
IC50 for the IKK complex is 200 nM
0.00004
4-(5-(3-amino-3-methyl-butyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
Homo sapiens
-
IC50 for the IKK complex is 40 nM
0.00005
4-(5-(3-hydroxy-3-methylbutyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amin
Homo sapiens
-
IC50 for the IKK complex is 50 nM, cellular profile
0.0001
4-(5-(3-methoxypropyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
Homo sapiens
-
IC50 for the IKK complex is 100 nM, cellular profile
0.00004
4-(5-(4-hydroxybutyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
Homo sapiens
-
IC50 for the IKK complex is 40 nM, cellular profile
0.0021 - 0.03
4-(5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)benzenesulfonamide
0.001 - 0.0251
4-(7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]isoquinolin-6-yl)benzenesulfonamide
0.0015 - 0.0025
4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)benzenesulfonamide
0.03
4-(piperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidin-2-amine
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.018
4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzoic acid
Homo sapiens
-
IC50 for the IKK complex is 0.018 mM, cellular profile
0.03
4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-amine
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.00013
4-methyl-7-methylamino-2-(azepan-1-yl)-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
Homo sapiens
-
IKK-2
0.000028 - 0.0026
4-methyl-7-methylamino-2-(methylthio)-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
0.0015
4-methyl-7-methylamino-2-benzylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
Homo sapiens
-
IKK-2
0.00016
4-methyl-7-methylamino-2-cyclopentylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
Homo sapiens
-
IKK-2
0.0025 - 0.02
4-methyl-7-methylamino-2-diethylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
0.000015 - 0.0011
4-methyl-7-methylamino-2-ethylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
0.0003
4-methyl-7-methylamino-2-hydroxyethylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
Homo sapiens
-
IKK-2
0.000015 - 0.00084
4-methyl-7-methylamino-2-methylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
0.00092 - 0.0034
4-methyl-7-methylamino-2-methylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
0.000011 - 0.00027
4-methyl-7-methylamino-2-phenyl-4H-imidazo[4,5-d]oxazolo[5,4-b]pyridine
0.000006 - 0.0035
4-methyl-7-methylamino-2-phenyl-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
0.00021 - 0.0061
4-methyl-7-methylamino-2-piperidine-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
0.000015
4-methyl-7-methylamino-2-thienylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
Homo sapiens
-
IKK-2
0.000033 - 0.0081
4-methyl-7-methylamino-2-[1,2,3,6-tetrahydropyridine]-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
0.0032 - 0.0251
4-[7-(benzyloxy)isoquinolin-6-yl]benzenesulfonamide
0.0008 - 0.005
4-[7-(piperidin-3-ylmethoxy)isoquinolin-6-yl]benzenesulfonamide
0.0008 - 0.0126
4-[7-(piperidin-3-yloxy)isoquinolin-6-yl]benzenesulfonamide
0.0006 - 0.0016
4-[7-(piperidin-4-ylmethoxy)isoquinolin-6-yl]benzenesulfonamide
0.0001 - 0.0079
4-[7-(piperidin-4-yloxy)isoquinolin-6-yl]benzenesulfonamide
0.0013 - 0.0251
4-[7-[(1-acetylpiperidin-4-yl)oxy]isoquinolin-6-yl]benzenesulfonamide
0.000011
4-[N'-(4,6-dimethylpyrimidin-2-yl)carbamimidamido]-N-(phenylcarbamoyl)benzene-1-sulfonamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0006
5,6-dibromo-beta-carboline
Homo sapiens
-
inhibits IKK with IC50 of 600 nM
0.0006
5-bromo-6-chloro-beta-carboline
Homo sapiens
-
inhibits IKK with IC50 of 600 nM
0.0011
5-bromo-6-cyano-beta-carboline
Homo sapiens
-
inhibits IKK with IC50 of 0.0011 mM
0.002
5-bromo-6-fluoro-beta-carboline
Homo sapiens
-
inhibits IKK with IC50 of 0.002 mM
0.004
5-bromo-6-methoxy-beta-carboline
Homo sapiens
-
nonspecific inhibitor of IKK, inhibits IKK with IC50 of 0.004 mM
0.0011
5-bromo-6-trifluoromethyl-beta-carboline
Homo sapiens
-
inhibits IKK with IC50 of 0.0011 mM
0.015
5-bromo-beta-carboline
Homo sapiens
-
inhibits IKK with IC50 of 0.015 mM
0.003
6,8-dichloro-7-(cyclohexylmethoxy)-9H-beta-carboline
Homo sapiens
-
inhibits IKK with IC50 of 0.003 mM
0.00014
6,8-dichloro-7-ethoxy-9H-beta-carboline
Homo sapiens
-
inhibits IKK with IC50 of 140 nM
0.00017
6,8-dichloro-7-methoxy-9H-beta-carboline
Homo sapiens
-
inhibits IKK with IC50 of 170 nM
0.0032
6,8-dichloro-9H-beta-carbolin-7-yl morpholine-4-carboxylate
Homo sapiens
-
inhibits IKK with IC50 of 0.0032 mM
0.0002
6,8-dichloro-beta-carboline
Homo sapiens
-
inhibits IKK with IC50 of 200 nM
0.0004 - 0.01
6-bromo-7-(piperidin-4-yloxy)isoquinoline
0.005 - 0.0251
6-bromo-7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]isoquinoline
0.0002 - 0.0032
6-phenyl-7-(piperidin-3-ylmethoxy)isoquinoline
0.0006 - 0.004
6-phenyl-7-(piperidin-3-yloxy)isoquinoline
0.0013 - 0.01
6-phenyl-7-(piperidin-4-ylmethoxy)isoquinoline
0.0001 - 0.0025
6-phenyl-7-(piperidin-4-yloxy)isoquinoline
0.004 - 0.0251
6-phenyl-7-(pyridin-3-ylmethoxy)isoquinoline
0.005 - 0.0251
6-phenyl-7-(pyridin-4-ylmethoxy)isoquinoline
0.000044
7-(2-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
Homo sapiens
-
0.000007
7-(3-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
Homo sapiens
-
0.000008
7-(3-methoxyphenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
Homo sapiens
-
0.000043 - 0.00173
7-(4-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
0.00008
7-(OCH2CH(CH2CH2))-6,8-dichloro-beta-carboline
Homo sapiens
-
inhibits IKK with IC50 of 80 nM
0.005 - 0.0251
7-(piperidin-4-yloxy)isoquinoline
0.011
7-hydroxy-6,8-dichloro-beta-carboline
Homo sapiens
-
inhibits IKK with IC50 of 0.011 mM
0.0126 - 0.0251
7-[(1-acetylpiperidin-4-yl)oxy]-6-bromoisoquinoline
0.0016 - 0.0032
7-[(1-acetylpiperidin-4-yl)oxy]-6-phenylisoquinoline
0.000011
7-[3-(aminomethyl)phenyl]-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
Homo sapiens
-
0.0025 - 0.02
7-[[1-(ethylsulfonyl)piperidin-4-yl]methoxy]-6-phenylisoquinoline
0.002 - 0.0126
7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]-6-phenylisoquinoline
0.00004 - 0.0141
8-(5-chloro-2-(4-methylpiperazin-1-yl)isonicotinamido)-1-(4-fluorophenyl)-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide
0.0013
8-amino-6-chloro-beta-carboline
Homo sapiens
-
inhibits IKK with IC50 of 0.0013 mM
0.0018
8-dimethylamino-6-chloro-beta-carboline
Homo sapiens
-
inhibits IKK with IC50 of 0.0018 mM
0.00018 - 0.02
8-methyl-2-(4-fluorophenyl)-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine
0.0018
8-methylamino-6-chloro-beta-carboline
Homo sapiens
-
inhibits IKK with IC50 of 0.0018 mM
0.004
8-nitro-6-chloro-beta-carboline
Homo sapiens
-
inhibits IKK with IC50 of 0.004 mM
0.000033 - 0.005
acetamide,N-[2-[[2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-yl]amino]ethyl]
0.000041
BX795
Homo sapiens
-
0.007
chalcone
Homo sapiens
-
0.000075 - 0.0086
ethanol,N-[2-[[2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-yl]amino]ethyl]
0.01681
lysyl-N-(4-methoxynaphthalen-2-yl)alaninamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0007
methyl (6-chloro-9H-beta-carbolin-8-yl)carbamate
Homo sapiens
-
inhibits IKK with IC50 of 700 nM
0.0078
methyl 1-(3-amino-2-carbamoyl-4-propylthieno[2,3-b]pyridin-6-yl)piperidine-4-carboxylate
Homo sapiens
-
IKKbeta
0.00004 - 0.00167
N,1-dimethyl-7-phenyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
0.000034 - 0.00099
N,1-dimethyl-7-phenyl-1H-pyrazolo[5,1-b]purin-4-amine
0.00052 - 0.00428
N,3,8-trimethyl-2-phenyl-3,8-dihydrodiimidazo[4,5-b:4',5'-d]pyridin-5-amine
0.000011 - 0.00027
N,8-dimethyl-2-phenyl-8H-imidazo[4,5-d][1,3]oxazolo[5,4-b]pyridin-5-amine
0.000006 - 0.0035
N,8-dimethyl-2-phenyl-8H-imidazo[4,5-d][1,3]thiazolo[5,4-b]pyridin-5-amine
0.0013 - 0.01
N,N-dimethyl-3-[(4-[[(6-phenylisoquinolin-7-yl)oxy]methyl]piperidin-1-yl)sulfonyl]propan-1-amine
0.0003 - 0.004
N-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)ethane-1,2-diamine
0.0044
N-(2-aminoethyl)-4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzamide
Homo sapiens
-
IC50 for the IKK complex is 0.0044 mM
0.0003
N-(2-dimethyl-aminoethyl)-4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzamide
Homo sapiens
-
IC50 300 nM for the IK cellular profile
0.0005
N-(2-pyrrolidin-1-yl-ethyl)-4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzamide
Homo sapiens
-
IC50 for the IKK complex is 500 nM
0.1
N-(3-methyl-butyl)-4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzamide
Homo sapiens
-
IC50 for the IKKbeta is above 0.1 mM
0.00326
N-(3-[2-imino-6-methyl-3-[(3-nitrophenyl)methyl]-4-oxo-1,2,3,4-tetrahydropyrimidin-5-yl]propyl)-4-methylbenzene-1-sulfonamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0004 - 0.0017
N-(4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)-methanesulfonamide
0.003
N-(6-chloro-9H-beta-carbolin-8-yl)-2-(pyridin-2-yl)acetamide
Homo sapiens
-
inhibits IKK with IC50 of 0.003 mM
0.02
N-(6-chloro-9H-beta-carbolin-8-yl)-2-methoxybenzamide
Homo sapiens
-
inhibits IKK with IC50 of 0.02 mM
0.0006
N-(6-chloro-9H-beta-carbolin-8-yl)-3-methoxybenzamide
Homo sapiens
-
inhibits IKK with IC50 of 600 nM
0.02
N-(6-chloro-9H-beta-carbolin-8-yl)-4-hydroxybutanamide
Homo sapiens
-
inhibits IKK with IC50 of 0.02 mM
0.0013
N-(6-chloro-9H-beta-carbolin-8-yl)-4-methoxybenzamide
Homo sapiens
-
inhibits IKK with IC50 of 0.0013 mM
0.0006
N-(6-chloro-9H-beta-carbolin-8-yl)acetamide
Homo sapiens
-
inhibits IKK with IC50 of 600 nM
0.0007
N-(6-chloro-9H-beta-carbolin-8-yl)benzamide
Homo sapiens
-
inhibits IKK with IC50 of 700 nM
0.02
N-(6-chloro-9H-beta-carbolin-8-yl)benzenesulfonamide
Homo sapiens
-
inhibits IKK with IC50 of 0.02 mM
0.0083
N-(6-chloro-9H-beta-carbolin-8-yl)methanesulfonamide
Homo sapiens
-
inhibits IKK with IC50 of 0.0083 mM
0.02
N-(6-chloro-9H-beta-carbolin-8-yl)morpholine-4-carboxamide
Homo sapiens
-
inhibits IKK with IC50 of 0.02 mM
0.001
N-(6-chloro-9H-beta-carbolin-8-yl)pyridine-2-carboxamide
Homo sapiens
-
inhibits IKK with IC50 of 0.001 mM
0.0003
N-(6-chloro-9H-beta-carbolin-8-yl)pyridine-4-carboxamide
Homo sapiens
-
inhibits IKK with IC50 of 300 nM
0.000019 - 0.0004
N-(8-methyl-2-phenylimidazo[1,2-a]thieno[3,2-e]pyrazin-5-yl)ethane-1,2-diamine
0.02
N-benzyl-6-chloro-9H-beta-carbolin-8-amine
Homo sapiens
-
inhibits IKK with IC50 of 0.02 mM
0.000039 - 0.0034
N-ethyl-2-(4-fluorophenyl)-N-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine
0.000026 - 0.0031
N-methyl-2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine
0.000039 - 0.00015
N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]-1,2,3-thiadiazole-4-carboxamide
0.000014 - 0.000633
N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]acetamide
0.000022
N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]butanediamide
Homo sapiens
-
0.00028 - 0.0097
N-[5-[4-(cyclopropylamino)-1-methyl-1H-pyrazolo[5,1-b]purin-7-yl]-2-fluorobenzyl]acetamide
0.000053 - 0.0035
N-[[2-fluoro-5-[8-methyl-5-methylamino-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]acetamide
0.000032 - 0.0042
N-[[2-fluoro-5-[8-methyl-5-methylamino-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]methanesulfonamide
0.000016 - 0.001
N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]-1,2,3-thiadiazole-5-amide
0.000022 - 0.0019
N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]acetamide
0.000025 - 0.0014
N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]isoxazole-5-amide
0.000005 - 0.001
N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]methanesulfonamide
0.000079
N2,N2-dimethyl-N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]glycinamide
Homo sapiens
-
0.03
N4-cyclohexyl-5-(trifluoromethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.03
N4-cyclohexyl-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.00037 - 0.00064
noraristeromycin
0.00001
PHA-408
Rattus norvegicus
-
less than 0.000010
0.0001
PS-1145
Homo sapiens
-
i.e. 8-(NHC(O)-3'-pyridyl)-6-chloro-beta-carboline, inhibits IKK with IC50 of 100 nM in vitro, blocks phosphorylation of IkappaBalpha and subsequent activation of NFkappaB in vivo
0.02
S1627
Homo sapiens
-
specific for the IKK complex, inhibits purified IKK in vitro with IC50 of 0.02 mM, inhibits IKK and NFkappaB nuclear translocation in vivo in umbilical vein endothelial cells and in rats, overview
-
0.0025
(R)-2-amino-4-(2-(hydroximethyl)pyrrolidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.03
(R)-2-amino-4-(2-(hydroximethyl)pyrrolidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.006
(R)-2-amino-4-(3-hydroxypyrrolidin-1-yl)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.03
(R)-2-amino-4-(3-hydroxypyrrolidin-1-yl)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.0031
(S)-2-amino-4-(2-(hydroximethyl)pyrrolidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.03
(S)-2-amino-4-(2-(hydroximethyl)pyrrolidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.00052
1,4-dimethyl-7-methylamino-2-phenyl-4H-imidazo[4,5-d]imidazo[5,4-b]pyridine
Homo sapiens
-
IKK-2
0.0043
1,4-dimethyl-7-methylamino-2-phenyl-4H-imidazo[4,5-d]imidazo[5,4-b]pyridine
Homo sapiens
-
IKK-1
0.0053
1-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-sulfonamide
Homo sapiens
at pH 7.5 and 30°C
0.0059
1-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-sulfonamide
Homo sapiens
at pH 7.5 and 30°C
0.0008
1-[3-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanamine
Homo sapiens
-
IKK-beta
0.0126
1-[3-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanamine
Homo sapiens
-
IKK-alpha
0.0001
1-[4-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanamine
Homo sapiens
-
IKK-beta
0.0063
1-[4-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanamine
Homo sapiens
-
IKK-alpha
0.0004
1-[4-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanesulfonamide
Homo sapiens
-
IKK-beta
0.004
1-[4-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanesulfonamide
Homo sapiens
-
IKK-alpha
0.000056
2-(4-fluorophenyl)-8-methyl-N-[2-(piperidin-1-yl)ethyl]-8H-imidazo[4,5-d][1,3]thiazolo[5,4-b]pyridin-5-amine
Homo sapiens
-
IKK-2
0.0083
2-(4-fluorophenyl)-8-methyl-N-[2-(piperidin-1-yl)ethyl]-8H-imidazo[4,5-d][1,3]thiazolo[5,4-b]pyridin-5-amine
Homo sapiens
-
IKK-1
0.0008
2-amino-4-((1R,2S,3R,4S)-2,3,4-trihydroxycyclopentylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.0036
2-amino-4-((1R,2S,3R,4S)-2,3,4-trihydroxycyclopentylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.002
2-amino-4-((1R,4R)-4-hydroxycyclohexylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.03
2-amino-4-((1R,4R)-4-hydroxycyclohexylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.001
2-amino-4-((1RS,2SR,3RS)-2,3-dihydroxycyclopentylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.03
2-amino-4-((1RS,2SR,3RS)-2,3-dihydroxycyclopentylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.016
2-amino-4-((cyclopropylmethyl)amino)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.03
2-amino-4-((cyclopropylmethyl)amino)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.002
2-amino-4-(2-fluorophenyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.03
2-amino-4-(2-fluorophenyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.0016
2-amino-4-(2-hydroxyethylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.03
2-amino-4-(2-hydroxyethylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.015
2-amino-4-(2-hydroxyphenyl)-77H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.03
2-amino-4-(2-hydroxyphenyl)-77H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.004
2-amino-4-(3-(hydroxymethyl)phenyl)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.0098
2-amino-4-(3-(hydroxymethyl)phenyl)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.0077
2-amino-4-(3-fluorophenyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.03
2-amino-4-(3-fluorophenyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.0121
2-amino-4-(3-hydroxypropylamino)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.03
2-amino-4-(3-hydroxypropylamino)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.0024
2-amino-4-(3-hydroyphenyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.0038
2-amino-4-(3-hydroyphenyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.0003
2-amino-4-(4-(methylsulfonyl)phenyl)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.0024
2-amino-4-(4-(methylsulfonyl)phenyl)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.01
2-amino-4-(4-fluorophenyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.03
2-amino-4-(4-fluorophenyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.00065
2-amino-4-(4-hydroxymethyl)phenyl-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.0023
2-amino-4-(4-hydroxymethyl)phenyl-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.0016
2-amino-4-(4-hydroxyphenyl)-7H-pyrrolo[2,3-d]pyrimdine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.02
2-amino-4-(4-hydroxyphenyl)-7H-pyrrolo[2,3-d]pyrimdine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.0053
2-amino-4-(benzylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.03
2-amino-4-(benzylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.0018
2-amino-4-(cyclohexylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.03
2-amino-4-(cyclohexylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.013
2-amino-4-(methylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.03
2-amino-4-(methylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.013
2-amino-4-(phenylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.03
2-amino-4-(phenylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.0053
2-amino-4-(piperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.03
2-amino-4-(piperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.004
2-amino-4-chloro-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.03
2-amino-4-chloro-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.02
2-amino-4-morpholino-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.03
2-amino-4-morpholino-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.0017
2-amino-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.03
2-amino-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.000081
2-methanesulfonyl-4-methyl-7-methylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
Homo sapiens
-
IKK-2
0.0076
2-methanesulfonyl-4-methyl-7-methylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
Homo sapiens
-
IKK-1
0.000009
2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7yl)pyridin-2-yl)methyl)acetamide
Homo sapiens
-
IKKbeta catalyzed phosphorylation of IkappaBalpha
0.00029
2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7yl)pyridin-2-yl)methyl)acetamide
Homo sapiens
-
IkappaBalpha phosphorylation in peripheral blood mononuclear cell
0.00496
2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7yl)pyridin-2-yl)methyl)acetamide
Homo sapiens
-
IKKalpha catalyzed phosphorylation of IkappaBalpha
0.0053
3-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-benzenesulfonamide
Homo sapiens
at pH 7.5 and 30°C
0.0059
3-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-benzenesulfonamide
Homo sapiens
at pH 7.5 and 30°C
0.00057
3-amino-6-(3-hydroxypiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.013
3-amino-6-(3-hydroxypiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
whole blood assay
0.0133
3-amino-6-(3-hydroxypiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKalpha
0.000041
3-amino-6-(4-aminopiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.00009
3-amino-6-(4-aminopiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKalpha
0.0016
3-amino-6-(4-aminopiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
whole blood assay
0.00028
3-amino-6-(4-hydroxypiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.0098
3-amino-6-(4-hydroxypiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
whole blood assay
0.0112
3-amino-6-(4-hydroxypiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKalpha
0.00012
3-amino-6-piperazin-1-yl-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKbeta
0.0032
3-amino-6-piperazin-1-yl-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
whole blood assay
0.0034
3-amino-6-piperazin-1-yl-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens
-
IKKalpha
0.000012
3-methoxy-N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]propanamide
Homo sapiens
-
0.00262
3-methoxy-N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]propanamide
Homo sapiens
-
0.0079
3-[7-(benzyloxy)isoquinolin-6-yl]benzenesulfonamide
Homo sapiens
-
IKK-beta
0.0251
3-[7-(benzyloxy)isoquinolin-6-yl]benzenesulfonamide
Homo sapiens
-
IKK-alpha, less than 0.0251
0.0013
3-[7-(piperidin-4-yloxy)isoquinolin-6-yl]benzenesulfonamide
Homo sapiens
-
IKK-beta
0.0079
3-[7-(piperidin-4-yloxy)isoquinolin-6-yl]benzenesulfonamide
Homo sapiens
-
IKK-alpha
0.01
4-((2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-benzenesulfonamide
Homo sapiens
at pH 7.5 and 30°C
0.03
4-((2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-benzenesulfonamide
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.016
4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimdin-4-yl)benzamide
Homo sapiens
at pH 7.5 and 30°C
0.03
4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimdin-4-yl)benzamide
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.00008
4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-benzenesulfonamide
Homo sapiens
at pH 7.5 and 30°C
0.001
4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-benzenesulfonamide
Homo sapiens
at pH 7.5 and 30°C
0.0014
4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-N-(p-tolyl)-benzenesulfonamide
Homo sapiens
at pH 7.5 and 30°C
0.016
4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-N-(p-tolyl)-benzenesulfonamide
Homo sapiens
at pH 7.5 and 30°C
0.0001
4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-N-methylbenzenesulfonamide
Homo sapiens
at pH 7.5 and 30°C
0.0014
4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-N-methylbenzenesulfonamide
Homo sapiens
at pH 7.5 and 30°C
0.00061
4-(2-amino-7H-pyrrol[2,3-d]pyrimidin-4-yl)benzenesulfonamide
Homo sapiens
at pH 7.5 and 30°C
0.0029
4-(2-amino-7H-pyrrol[2,3-d]pyrimidin-4-yl)benzenesulfonamide
Homo sapiens
at pH 7.5 and 30°C
0.0021
4-(5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)benzenesulfonamide
Homo sapiens
at pH 7.5 and 30°C
0.03
4-(5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)benzenesulfonamide
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.001
4-(7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]isoquinolin-6-yl)benzenesulfonamide
Homo sapiens
-
IKK-beta
0.0251
4-(7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]isoquinolin-6-yl)benzenesulfonamide
Homo sapiens
-
-
0.0015
4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)benzenesulfonamide
Homo sapiens
at pH 7.5 and 30°C
0.0025
4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)benzenesulfonamide
Homo sapiens
at pH 7.5 and 30°C
0.000028
4-methyl-7-methylamino-2-(methylthio)-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
Homo sapiens
-
IKK-2
0.0026
4-methyl-7-methylamino-2-(methylthio)-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
Homo sapiens
-
IKK-1
0.0025
4-methyl-7-methylamino-2-diethylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
Homo sapiens
-
IKK-2
0.02
4-methyl-7-methylamino-2-diethylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
Homo sapiens
-
IKK-1
0.000015
4-methyl-7-methylamino-2-ethylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
Homo sapiens
-
IKK-2
0.0011
4-methyl-7-methylamino-2-ethylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
Homo sapiens
-
IKK-1
0.000015
4-methyl-7-methylamino-2-methylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
Homo sapiens
-
IKK-2
0.00084
4-methyl-7-methylamino-2-methylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
Homo sapiens
-
IKK-1
0.00092
4-methyl-7-methylamino-2-methylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
Homo sapiens
-
IKK-2
0.0034
4-methyl-7-methylamino-2-methylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
Homo sapiens
-
IKK-1
0.000011
4-methyl-7-methylamino-2-phenyl-4H-imidazo[4,5-d]oxazolo[5,4-b]pyridine
Homo sapiens
-
IKK-2
0.00027
4-methyl-7-methylamino-2-phenyl-4H-imidazo[4,5-d]oxazolo[5,4-b]pyridine
Homo sapiens
-
IKK-1
0.000006
4-methyl-7-methylamino-2-phenyl-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
Homo sapiens
-
IKK-2
0.0035
4-methyl-7-methylamino-2-phenyl-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
Homo sapiens
-
IKK-1
0.00021
4-methyl-7-methylamino-2-piperidine-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
Homo sapiens
-
IKK-2
0.0061
4-methyl-7-methylamino-2-piperidine-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
Homo sapiens
-
IKK-1
0.000033
4-methyl-7-methylamino-2-[1,2,3,6-tetrahydropyridine]-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
Homo sapiens
-
IKK-2
0.0081
4-methyl-7-methylamino-2-[1,2,3,6-tetrahydropyridine]-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
Homo sapiens
-
IKK-1
0.0032
4-[7-(benzyloxy)isoquinolin-6-yl]benzenesulfonamide
Homo sapiens
-
IKK-beta
0.0251
4-[7-(benzyloxy)isoquinolin-6-yl]benzenesulfonamide
Homo sapiens
-
IKK-alpha, less than 0.0251
0.0008
4-[7-(piperidin-3-ylmethoxy)isoquinolin-6-yl]benzenesulfonamide
Homo sapiens
-
IKK-beta
0.005
4-[7-(piperidin-3-ylmethoxy)isoquinolin-6-yl]benzenesulfonamide
Homo sapiens
-
IKK-alpha
0.0008
4-[7-(piperidin-3-yloxy)isoquinolin-6-yl]benzenesulfonamide
Homo sapiens
-
IKK-beta
0.0126
4-[7-(piperidin-3-yloxy)isoquinolin-6-yl]benzenesulfonamide
Homo sapiens
-
IKK-alpha
0.0006
4-[7-(piperidin-4-ylmethoxy)isoquinolin-6-yl]benzenesulfonamide
Homo sapiens
-
IKK-beta
0.0016
4-[7-(piperidin-4-ylmethoxy)isoquinolin-6-yl]benzenesulfonamide
Homo sapiens
-
IKK-alpha
0.0001
4-[7-(piperidin-4-yloxy)isoquinolin-6-yl]benzenesulfonamide
Homo sapiens
-
IKK-beta
0.0079
4-[7-(piperidin-4-yloxy)isoquinolin-6-yl]benzenesulfonamide
Homo sapiens
-
IKK-alpha
0.0013
4-[7-[(1-acetylpiperidin-4-yl)oxy]isoquinolin-6-yl]benzenesulfonamide
Homo sapiens
-
IKK-beta
0.0251
4-[7-[(1-acetylpiperidin-4-yl)oxy]isoquinolin-6-yl]benzenesulfonamide
Homo sapiens
-
IKK-alpha, less than 0.0251
0.0004
6-bromo-7-(piperidin-4-yloxy)isoquinoline
Homo sapiens
-
IKK-beta
0.01
6-bromo-7-(piperidin-4-yloxy)isoquinoline
Homo sapiens
-
IKK-alpha
0.005
6-bromo-7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]isoquinoline
Homo sapiens
-
IKK-beta
0.0251
6-bromo-7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]isoquinoline
Homo sapiens
-
IKK-alpha, less than 0.0251
0.0002
6-phenyl-7-(piperidin-3-ylmethoxy)isoquinoline
Homo sapiens
-
IKK-beta
0.0032
6-phenyl-7-(piperidin-3-ylmethoxy)isoquinoline
Homo sapiens
-
IKK-alpha
0.0006
6-phenyl-7-(piperidin-3-yloxy)isoquinoline
Homo sapiens
-
IKK-beta
0.004
6-phenyl-7-(piperidin-3-yloxy)isoquinoline
Homo sapiens
-
IKK-alpha
0.0013
6-phenyl-7-(piperidin-4-ylmethoxy)isoquinoline
Homo sapiens
-
IKK-beta
0.01
6-phenyl-7-(piperidin-4-ylmethoxy)isoquinoline
Homo sapiens
-
IKK-alpha
0.0001
6-phenyl-7-(piperidin-4-yloxy)isoquinoline
Homo sapiens
-
IKK-beta
0.0025
6-phenyl-7-(piperidin-4-yloxy)isoquinoline
Homo sapiens
-
IKK-alpha
0.004
6-phenyl-7-(pyridin-3-ylmethoxy)isoquinoline
Homo sapiens
-
IKK-beta
0.0251
6-phenyl-7-(pyridin-3-ylmethoxy)isoquinoline
Homo sapiens
-
IKK-alpha, less than 0.0251
0.005
6-phenyl-7-(pyridin-4-ylmethoxy)isoquinoline
Homo sapiens
-
IKK-beta
0.0251
6-phenyl-7-(pyridin-4-ylmethoxy)isoquinoline
Homo sapiens
-
IKK-alpha, less than 0.0251
0.000043
7-(4-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
Homo sapiens
-
0.00173
7-(4-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
Homo sapiens
-
0.005
7-(piperidin-4-yloxy)isoquinoline
Homo sapiens
-
IKK-beta
0.0251
7-(piperidin-4-yloxy)isoquinoline
Homo sapiens
-
IKK-alpha, less than 0.0251
0.0126
7-[(1-acetylpiperidin-4-yl)oxy]-6-bromoisoquinoline
Homo sapiens
-
IKK-beta
0.0251
7-[(1-acetylpiperidin-4-yl)oxy]-6-bromoisoquinoline
Homo sapiens
-
IKK-alpha, less than 0.0251
0.0016
7-[(1-acetylpiperidin-4-yl)oxy]-6-phenylisoquinoline
Homo sapiens
-
IKK-alpha
0.0032
7-[(1-acetylpiperidin-4-yl)oxy]-6-phenylisoquinoline
Homo sapiens
-
IKK-beta
0.0025
7-[[1-(ethylsulfonyl)piperidin-4-yl]methoxy]-6-phenylisoquinoline
Homo sapiens
-
IKK-beta
0.02
7-[[1-(ethylsulfonyl)piperidin-4-yl]methoxy]-6-phenylisoquinoline
Homo sapiens
-
IKK-alpha
0.002
7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]-6-phenylisoquinoline
Homo sapiens
-
IKK-beta
0.0126
7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]-6-phenylisoquinoline
Homo sapiens
-
IKK-alpha
0.00004
8-(5-chloro-2-(4-methylpiperazin-1-yl)isonicotinamido)-1-(4-fluorophenyl)-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide
Homo sapiens
-
0.0141
8-(5-chloro-2-(4-methylpiperazin-1-yl)isonicotinamido)-1-(4-fluorophenyl)-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide
Homo sapiens
-
0.00018
8-methyl-2-(4-fluorophenyl)-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine
Homo sapiens
-
IKK-2
0.02
8-methyl-2-(4-fluorophenyl)-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine
Homo sapiens
-
IKK-1, larger than 0.020
0.000033
acetamide,N-[2-[[2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-yl]amino]ethyl]
Homo sapiens
-
IKK-2
0.005
acetamide,N-[2-[[2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-yl]amino]ethyl]
Homo sapiens
-
IKK-1
0.000075
ethanol,N-[2-[[2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-yl]amino]ethyl]
Homo sapiens
-
IKK-2
0.0086
ethanol,N-[2-[[2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-yl]amino]ethyl]
Homo sapiens
-
IKK-1
0.00004
N,1-dimethyl-7-phenyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
Homo sapiens
-
0.00167
N,1-dimethyl-7-phenyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
Homo sapiens
-
0.000034
N,1-dimethyl-7-phenyl-1H-pyrazolo[5,1-b]purin-4-amine
Homo sapiens
-
IKK-2
0.00099
N,1-dimethyl-7-phenyl-1H-pyrazolo[5,1-b]purin-4-amine
Homo sapiens
-
IKK-1
0.00052
N,3,8-trimethyl-2-phenyl-3,8-dihydrodiimidazo[4,5-b:4',5'-d]pyridin-5-amine
Homo sapiens
-
0.00428
N,3,8-trimethyl-2-phenyl-3,8-dihydrodiimidazo[4,5-b:4',5'-d]pyridin-5-amine
Homo sapiens
-
0.000011
N,8-dimethyl-2-phenyl-8H-imidazo[4,5-d][1,3]oxazolo[5,4-b]pyridin-5-amine
Homo sapiens
-
0.00027
N,8-dimethyl-2-phenyl-8H-imidazo[4,5-d][1,3]oxazolo[5,4-b]pyridin-5-amine
Homo sapiens
-
0.000006
N,8-dimethyl-2-phenyl-8H-imidazo[4,5-d][1,3]thiazolo[5,4-b]pyridin-5-amine
Homo sapiens
-
0.0035
N,8-dimethyl-2-phenyl-8H-imidazo[4,5-d][1,3]thiazolo[5,4-b]pyridin-5-amine
Homo sapiens
-
0.0013
N,N-dimethyl-3-[(4-[[(6-phenylisoquinolin-7-yl)oxy]methyl]piperidin-1-yl)sulfonyl]propan-1-amine
Homo sapiens
-
IKK-beta
0.01
N,N-dimethyl-3-[(4-[[(6-phenylisoquinolin-7-yl)oxy]methyl]piperidin-1-yl)sulfonyl]propan-1-amine
Homo sapiens
-
IKK-alpha
0.0003
N-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)ethane-1,2-diamine
Homo sapiens
-
IKK-2
0.004
N-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)ethane-1,2-diamine
Homo sapiens
-
IKK-1
0.0004
N-(4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)-methanesulfonamide
Homo sapiens
at pH 7.5 and 30°C
0.0017
N-(4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)-methanesulfonamide
Homo sapiens
at pH 7.5 and 30°C
0.000019
N-(8-methyl-2-phenylimidazo[1,2-a]thieno[3,2-e]pyrazin-5-yl)ethane-1,2-diamine
Homo sapiens
-
IKK-2
0.0004
N-(8-methyl-2-phenylimidazo[1,2-a]thieno[3,2-e]pyrazin-5-yl)ethane-1,2-diamine
Homo sapiens
-
IKK-1
0.000039
N-ethyl-2-(4-fluorophenyl)-N-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine
Homo sapiens
-
IKK-2
0.0034
N-ethyl-2-(4-fluorophenyl)-N-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine
Homo sapiens
-
IKK-1
0.000026
N-methyl-2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine
Homo sapiens
-
IKK-2
0.0031
N-methyl-2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine
Homo sapiens
-
IKK-1
0.000039
N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]-1,2,3-thiadiazole-4-carboxamide
Homo sapiens
-
0.00015
N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]-1,2,3-thiadiazole-4-carboxamide
Homo sapiens
-
0.000014
N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]acetamide
Homo sapiens
-
0.000633
N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]acetamide
Homo sapiens
-
0.00028
N-[5-[4-(cyclopropylamino)-1-methyl-1H-pyrazolo[5,1-b]purin-7-yl]-2-fluorobenzyl]acetamide
Homo sapiens
-
IKK-2
0.0097
N-[5-[4-(cyclopropylamino)-1-methyl-1H-pyrazolo[5,1-b]purin-7-yl]-2-fluorobenzyl]acetamide
Homo sapiens
-
IKK-1
0.000053
N-[[2-fluoro-5-[8-methyl-5-methylamino-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]acetamide
Homo sapiens
-
IKK-2
0.0035
N-[[2-fluoro-5-[8-methyl-5-methylamino-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]acetamide
Homo sapiens
-
IKK-1
0.000032
N-[[2-fluoro-5-[8-methyl-5-methylamino-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]methanesulfonamide
Homo sapiens
-
IKK-2
0.0042
N-[[2-fluoro-5-[8-methyl-5-methylamino-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]methanesulfonamide
Homo sapiens
-
IKK-1
0.000016
N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]-1,2,3-thiadiazole-5-amide
Homo sapiens
-
IKK-2
0.001
N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]-1,2,3-thiadiazole-5-amide
Homo sapiens
-
IKK-1
0.000022
N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]acetamide
Homo sapiens
-
IKK-2
0.0019
N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]acetamide
Homo sapiens
-
IKK-1
0.000025
N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]isoxazole-5-amide
Homo sapiens
-
IKK-2
0.0014
N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]isoxazole-5-amide
Homo sapiens
-
IKK-1
0.000005
N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]methanesulfonamide
Homo sapiens
-
IKK-2
0.001
N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]methanesulfonamide
Homo sapiens
-
IKK-1
0.00037
noraristeromycin
Homo sapiens
-
IKKalpha
0.00064
noraristeromycin
Homo sapiens
-
inhibited endogenous IKK activity following TNF-alpha stimulation
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C99S
the mutation partially abolishes (E)-2-methoxy-4-(3-(4-methoxyphenyl)prop-1-en-1-yl)phenol-induced cell growth inhibition and enhances expression of death receptors 5 and 6
D145A
site-directed mutagenesis, the IKK-2 is devoid of kinase activity despite its ability to bind ATP with high affinity and is not phosphorylated at the T loop. mutant binds a diverse collection of inhibitors with comparable binding affinities to wild-type IKK-2, inhibition by PHA-408 is reduced compared to the wild-type enzyme
DELTA1-640
deletion mutant containing residues 640-756, which contains the entire C-terminal region after the HLH domain, interacts well with NEMO
DELTA1-680
deletion mutant wich stably interacts with NEMO
DELTA1-705
deletion mutant comprising just the predicted alpha-helical and coiled-coil region and the NEMO binding domain (NPD) residues 734-745 is sufficient for a stable interaction with NEMO
DELTA1-734
deletion mutant containing only the 11-residues of the NEMO-binding region (NBD) is not sufficient for interaction with NEMO
DELTA307-384
mutant protein consisting of a deletion of the ubiquitin-like domain that is present only in IKKbeta fails to activate NFkappaB in response to IL-1 or TNF. Deletion mutant is incorporated into the IKK complex, indicating that this domain is not important for the intermolecular interaction between the IKKs and NEMO. Deletion mutant strongly associate with the NF-kappaB p65 subunit in the absence or presence of stimuli, whereas wild-type IKKbeta can not be detected in a complex with p65. This indicates that the to propose a model in which the ubiquitin-like domain plays a role in release of NF-kappaB following IkappaBalpha phosphorylation
DELTA395-756
mutant lacking the leucine zipper domain, the helix-loop-helix domain, the serine rich and the NEMO-binding motif are capable to catalyze phosphotransfer to the substrate protein IkappaBalpha, but they do so at positions outside Ser-32 and Ser-36 while leaving these two critical amino acids unmodified. Removal of the leucine zipper and helix-loop-helix regions converts IKKbeta to monomer
DELTA395-756D145N
mutant lacking the leucine zipper domain, the helix-loop-helix domain, the serine rich and the NEMO-binding motif and containing a Asp145Asn mutation does not display any kinase activity
DELTA665-756
mutant lacking the serine rich and the NEMO-binding motif retains the ability to phosphorylate its substrate IkappaBalpha exclusively at serine positions 32 and 36
F26A
site-directed mutagenesis, the mutant has lost the time-dependent binding of inhibitor PHA-408
F26W
site-directed mutagenesis
K106N
site-directed mutagenesis
K106Q
site-directed mutagenesis, the mutant shows time-dependent inhibition like the wild-type, inhibition by PHA-408 is slightly increased compared to the wild-type enzyme
K106R
-
site-directed mutagenesis, ubiquitination and phosphorylation of the mutant is unaltered compared to the wild-type IKKbeta
K147R
-
site-directed mutagenesis, reduced monoubiquitination of IKKbeta mutant
K163R
-
site-directed mutagenesis, monoubiquitination-defective mutant of IKKbeta retaining kinase activity in Tax-expressing cells
K171R
-
site-directed mutagenesis, ubiquitination and phosphorylation of the mutant is unaltered compared to the wild-type IKKbeta
K18R
-
site-directed mutagenesis, ubiquitination and phosphorylation of the mutant is unaltered compared to the wild-type IKKbeta
K198R
-
site-directed mutagenesis, ubiquitination and phosphorylation of the mutant is unaltered compared to the wild-type IKKbeta
K234R
-
site-directed mutagenesis, ubiquitination and phosphorylation of the mutant is unaltered compared to the wild-type IKKbeta
K238R
-
site-directed mutagenesis, monoubiquitination-defective mutant of IKKbeta
K254R
-
site-directed mutagenesis, ubiquitination and phosphorylation of the mutant is unaltered compared to the wild-type IKKbeta
K275R
-
site-directed mutagenesis, ubiquitination and phosphorylation of the mutant is unaltered compared to the wild-type IKKbeta
K44A
-
site-directed mutagenesis of subunit IKK2, catalytically inactive mutant and no NF-kappaB stimulation in infected cells in vivo
K44R
-
site-directed mutagenesis, monoubiquitination-defective mutant of IKKbeta
L353X
L353 within the ubiquitin-like domain is necessary to activate NF-kappaB-dependent gene expression. However, the L353 mutant is able to phosphorylate IkappaBalpha suggesting that the defect in NF-kappaB activation is not at the level of inhibition of IkappaB degradation
L605R/F606P
-
IKKalpha mutant, defective in HLH domains, unable to bind wild-type Vav-1
M96L
site-directed mutagenesis
P191A
-
inactive IKKbeta mutant
S176E/S180E
-
vaccinia virus virulence factor B14 does inhibit a mutant containing a mutation in the activation loop. This suggests that phosphorylation of these serine residues in the activation loop of IKKbeta is targeted by B14
T23A
overexpression of a Ikappa B kinase alpha mutant, IKKalphaT23A, containing a mutation in a functional AKT phosphorylation site, completely abrogate IL-6 promoter activation in response to IL-1
Y169F
site-directed mutagenesis, the mutant shows time-dependent inhibition by PHA-408 like the wild-type
K38A
-
inactive IKKepsilon mutant
S177E/S181E
-
site-directed mutagenesis, gain-of-function mutant of IKK2, IKK2-EE or IKK2CA, the mutant ICC2CA in pancreatic acinar cells increases tissue damage of secretagogue induced experimental pancreatitits, overview
S176E/S180E
overexpression of a constitutively active IKKalpha-EGFP fusion protein shows that IKKalpha is sufficient to activate NF-kappaB activity and induce fiber atrophy in muscle
S177E/S181E
overexpression of a constitutively active IKKbeta-EGFP show a marked increase in NF-kappaB activity and a decrease in fiber size of weight-bearing soleus muscles, while muscles overexpressing wild-type IKKbeta-HA have no effect
C179A
-
site-directed mutagenesis of IKKbeta at the activation loop, the mutant shows reduced activation and activity compared to the wild-type enzyme, which is not restorable by TNF stimulation, activity of the mutant is partially recovered when its phosphorylation is enforced by coexpression with mitogen-activated protein kinase kinase kinases such as NF-kappaB inducing kinase, NIK, and MAPK/extracellular signal-regulated kinase kinase kinase 1, MEKK1, or when the serine residues are replaced with phospho-mimetic glutamate, the mutant is normal in dimer formation, while its activity abnormally responds to the change in the concentration of substrate ATP, overview
C179A
berberine does not have any effect on mutant IKK beta C179A. This proves that berberine inhibits IKK beta activity through the modification of Cys179
C179A
-
mutant, not susceptible to the inhibitor N-tosyl-L-phenylalanine chloromethyl ketone
K44M
-
site-directed mutagenesis, inactive IKKalpha mutant
K44M
-
site-directed mutagenesis, inactive IKKbeta mutant
K44M
-
a kinase-dead mutant of IKKalpha
S177E/S181E
ectopic overexpression of a constitutively active form of IKKbeta in Type II epithelial ovarian cancer cells (EOC) results in a significant decrease in IkappaBalpha expression
S177E/S181E
-
vaccina virus virulence factor B14 does not inhibit a mutant containing a mutation in the activation loop. This suggests that phosphorylation of these serine residues in the activation loop of IKKbeta is targeted by vaccina virus virulence factor B14
K44A
-
inactive IKKbeta mutant
K44A
-
site-directed mutagenesis, inactive ATP-binding site mutant, the kinase-deficient mutant IKK-alpha fails to stabilize p73
K44M
gene transfer of a dominant negative (kinase-dead form) IKKbeta into rat soleus muscles show complete inhibition of 7-day disuse-induced activation of a kappaB reporter gene, while overexpression of wild-type IKKbeta does not. Overexpression of a dominant-negative mutant IKKbeta-EGFP fusion protein show that atrophy is inhibited by 50%, indicating that IKKbeta is required for the atrophy process
K44M
overexpression of a dominant negative (kinase-dead form) IKKbeta plus dominant-negative IKKalpha show an additive effect on the inhibition of disuse atrophy (70%), suggesting that both kinases of the IKK complex are required for muscle atrophy
K44M
overexpression of a dominat-negative (kinase-dead form) of the IKKalpha protein decreases unloading-induced NF-kappaB activation and inhibits atrophy by 50%, while overexpression of the wild-type protein has no effect
additional information
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construction of IKKgamma peptide fragements and sequence deletion mutants for determination of intermolecular interaction of IKKgamma required for 2-step tetramerization, overview
additional information
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IKKepsilon and TBK1 interference RNA blocks IRF3 activation
additional information
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mutations of X-linked gene encoding IKKgamma can lead to immunodeficiency diseases interfering with NFkappaB-signaling
additional information
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IKK subunit-specific small interfering RNAs and cells deficient in individual IKK subunits show that IKKalpha subunit, not IKKbeta, is required for reovirus-induced NF-kappaB activation and apoptosis, overview, NF-kappaB activation and apoptosis are delayed in cells deficient in the IKK complex components IKKgamma/NEMO, overview
additional information
analysis of IKKalpha and IKKbeta knockout cells shows that IKK alpha is the critical IKK subunit in controlling insulin-induced interaction with mTOR
additional information
ectopic expression of IKKbeta in epithelial ovarian cancer cells (EOC) induces cytokine production in Type II EOC cells
additional information
ectopic expression of IKKbeta in epithelial ovarian cancer cells (EOC) induces cytokine production in Type II EOC cells
additional information
-
ectopic expression of IKKbeta in epithelial ovarian cancer cells (EOC) induces cytokine production in Type II EOC cells
additional information
enhanced IKKalpha expression increases both early and terminal differentiation of human keratinocytes through an E-cadherin-dependent mechanism
additional information
-
enhanced IKKalpha expression increases both early and terminal differentiation of human keratinocytes through an E-cadherin-dependent mechanism
additional information
expression of IKKalpha or IKKbeta is ablated in primary human chondrocytes by retrotransduction of specific short-hairpin RNAs. Micromass cultures designed to reproduce chondrogenesis with progression to the terminal hypertrophic stage are established, and anabolism and remodeling of the extracellular matrix (ECM) are investigated in the micromasses. Ablation of IKKalpha dramatically enhance type II collagen deposition independent of SOX9 protein levels but in association with suppressed levels of runt-related transcription factor 2. IKKalpha-deficient cells retain the phenotype of cells in a pre-hypertrophic-like state, as evidenced by the smaller size and faster proliferation of these cells prior to micromass seeding, along with the enhanced viability of their differentiated micromasses
additional information
expression of IKKalpha or IKKbeta is ablated in primary human chondrocytes by retrotransduction of specific short-hairpin RNAs. Micromass cultures designed to reproduce chondrogenesis with progression to the terminal hypertrophic stage are established, and anabolism and remodeling of the extracellular matrix (ECM) are investigated in the micromasses. Ablation of IKKalpha dramatically enhance type II collagen deposition independent of SOX9 protein levels but in association with suppressed levels of runt-related transcription factor 2. IKKalpha-deficient cells retain the phenotype of cells in a pre-hypertrophic-like state, as evidenced by the smaller size and faster proliferation of these cells prior to micromass seeding, along with the enhanced viability of their differentiated micromasses
additional information
-
expression of IKKalpha or IKKbeta is ablated in primary human chondrocytes by retrotransduction of specific short-hairpin RNAs. Micromass cultures designed to reproduce chondrogenesis with progression to the terminal hypertrophic stage are established, and anabolism and remodeling of the extracellular matrix (ECM) are investigated in the micromasses. Ablation of IKKalpha dramatically enhance type II collagen deposition independent of SOX9 protein levels but in association with suppressed levels of runt-related transcription factor 2. IKKalpha-deficient cells retain the phenotype of cells in a pre-hypertrophic-like state, as evidenced by the smaller size and faster proliferation of these cells prior to micromass seeding, along with the enhanced viability of their differentiated micromasses
additional information
expression of IKKalpha or IKKbeta is ablated in primary human chondrocytes by retrotransduction of specific short-hairpin RNAs. Silencing of IKKbeta markedly enhances accumulation of glycosaminoglycan in conjunction with increased SOX9 expression
additional information
expression of IKKalpha or IKKbeta is ablated in primary human chondrocytes by retrotransduction of specific short-hairpin RNAs. Silencing of IKKbeta markedly enhances accumulation of glycosaminoglycan in conjunction with increased SOX9 expression
additional information
-
expression of IKKalpha or IKKbeta is ablated in primary human chondrocytes by retrotransduction of specific short-hairpin RNAs. Silencing of IKKbeta markedly enhances accumulation of glycosaminoglycan in conjunction with increased SOX9 expression
additional information
-
in cells infected with vaccina virus lacking gene B14R there is a higher level of phosphorylated IkappaBalpha but a similar level of IkappaBalpha compared to cells infected with control viruses expressing vaccina virus virulence factor B14, suggesting vaccina virus virulence factor B14 affects IKK activity
additional information
-
in cells infected with vaccinia virus lacking gene B14R there is a higher level of phosphorylated IkappaBalpha but a similar level of IkappaBalpha compared to cells infected with control viruses expressing vaccinia virus virulence factor B14, suggesting vaccinia virus virulence factor B14 affects IKK activity
additional information
in HEK293 cells, knockdown of IKK alpha suppresses TNF-induced mTOR activation by greater that 50%, knockdown of IKKbeta has less of an effect
additional information
knockdown of IKKalpha alone or combined IKKalpha/beta causes significant loss of NF-kappaB DNA binding activity in Panc-1 cells. The suppressive effects of IKKalpha and combined IKKalpha/beta knockdown are stronger than IKKbeta knockdown alone
additional information
knockdown of IKKalpha alone or combined IKKalpha/beta causes significant loss of NF-kappaB DNA binding activity in Panc-1 cells. The suppressive effects of IKKalpha and combined IKKalpha/beta knockdown are stronger than IKKbeta knockdown alone
additional information
knockdown of IKKalpha and IKKbeta by RNAi leads to a significant reduction of Panc-1 cell and MiaPaCa-2 cell growth
additional information
knockdown of IKKalpha and IKKbeta by RNAi leads to a significant reduction of Panc-1 cell and MiaPaCa-2 cell growth
additional information
siRNA-directed knockdown of Akt2 in PC3 cells leads to dissociation of IKKalpha from the mTOR (mammalian target of rapamycin) complex
additional information
siRNA-directed knockdown of Akt2 in PC3 cells leads to dissociation of IKKalpha from the mTOR (mammalian target of rapamycin) complex
additional information
using siRNA to IKKalpha it is shown that IKKalpha is required for efficient induction of mTOR activation in response to insulin or TNF. Knockout of IKKalpha significantly reduces insulin- or TNF-induced activation
additional information
-
a vector expressing a mutant form of IKK2 is used, characterized by the substitution of two serine residues with alanines, leading to inhibition of IKK2 autophosphorylation required for IKK activity
additional information
-
overexpressing a dominant-negative mutant of IKKbeta in 38E6E7HFK cells results in reduced levels of phospho-IkappaBalpha and a decrease in DELTANp73alpha protein levels, while no significant changes in DELTANp73alpha mRNA levels are observed
additional information
-
construction of IKK knockout mice as a model system for drug development
additional information
-
construction of IKKalpha-deficient and of IKKbeta-deficient mice and BM cell mutants, the mutants show defective osteoclastogenesis, wild-type osteoblasts can rescue osteoclastogenesis in IKKalpha- and IKKbeta-defective mutant BM cells, exogenic TNFalpha can rescue only IKKalpha-deficient mutants, TNFR1 can rescue IKKbeta-deficient osteoclast progenitors, but not prevent TNFalpha-induced apoptosis, overview
additional information
-
disruption of the gene encoding IKKbeta leads to apoptotic tissue damage, e.g. in mucosa, and prevention of systemic inflammatory response, which results in the multiple organ dysfunction syndrome MODS
additional information
-
IKKbeta-deficient B-cells are impaired in mitogenic responses to lipopolysaccharides, anti-CD40, and anti-IgM, and show high reduction of all peripheral B-cell subsets due to associated defects in cell survival
additional information
-
disruption of Ikbke-/-, the gene encoding IKKepsilon, results in a complete loss of the kinase in both mice and embryonic fibroblasts, generation of mice lacking IKKepsilon, the mice produce normal amounts of IFNbeta, but are hypersusceptible to viral infection because of a defect in the IFN signaling pathway, phenotype, overview
additional information
-
fibroblasts of ikkbeta-/- mice exhibit enhanced apoptosis in response to TNFalpha, NEMO/IKKgamma-deficient mice shows a phenotype with liver damage, but can be rescued by inactivation of the gene encoding the tumor necrosis factor-1, phenotypes, overview
additional information
-
generation of IKKalpha-/- mice, an autoimmune disease phenotype is induced in athymic nude mice by grafting embryonic thymus from IKKalpha-deficient mice
additional information
-
IKK knockout mice show downregulation of the CBM complex components Carma1 and Malt1, and impaired degradation of IkappaBalpha, overview
additional information
-
IkkalphaAA/AA 'knockin' mice, in which activation of IKKalpha is prevented by replacement of activation loop serines with alanines, exhibit delayed mammary gland growth during pregnancy, because IKKalpha activity is required for cyclin D1 induction and proliferation of lobuloalveolar epithelial cells, overview, retarded tumor development in response to either 7,12-dimethylbenzaanthracene or the ErbB2/Her2 transgene but had no effect on MMTV-v-Haras-induced cancer, overview
additional information
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IKKbeta-/- 3T3 fibroblasts show decreased expression of antioxidant genes, such as metallothionein 1, Mt1, IKKbeta null cells display a marked increase in arsenic-induced reactive oxygen species accumulation, which leads to activation of the MKK4-c-Jun NH2-terminal kinase pathway, c-Jun phosphorylation, and apoptosis, overview
additional information
-
small interfering RNA-mediated knockdown of endogenous IKK-alpha inhibits the CDDP-mediated accumulation of p73alpha, the kinase-deficient mutant form of IKK-alpha interacts with p73alpha, but fails to stabilize it, CDDP-mediated accumulation of endogenous p73alpha is not detected in mouse embryonic fibroblasts prepared from IKK-alpha-deficient mice, and CDDP sensitivity is significantly decreased compared to wild-type MEFs, overview
additional information
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TLR7/9-induced IFN-alpha production is severely impaired in constructed IKK-alpha-deficient plasmacytoid dendritic cells, whereas inflammatory cytokine induction is decreased but still occurrs, kinase-deficient IKK-alpha inhibits the ability of MyD88 to activate the Ifna promoter in synergy with IRF-7, expression of kinase-deficient IKK-alpha does not affect IRF-7-mediated promoter activation, but inhibits the enhancing effects ofMyD88
additional information
-
transfection of siRNA duplexes directed against IKKi and TBK1 downregulates the expression levels of both kinase isoforms by about 70%
additional information
conditional IKKbeta knockout mice are used in which the IKKbeta gene is specifically deleted in cells of myeloid lineage, including microglia, in the CNS. This deletion reduced IkappaB kinase (IKK) activity in cultured primary microglia by up to 40% compared with wild-type. Kainic acid-induced hippocampal neuronal cell death is reduced by 30% in knockout mice compared with wild-type mice
additional information
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conditional IKKbeta knockout mice are used in which the IKKbeta gene is specifically deleted in cells of myeloid lineage, including microglia, in the CNS. This deletion reduced IkappaB kinase (IKK) activity in cultured primary microglia by up to 40% compared with wild-type. Kainic acid-induced hippocampal neuronal cell death is reduced by 30% in knockout mice compared with wild-type mice
additional information
gene disruption via homologous recombination reveals that activation of NF-kappaB in response to pathogen associated molecular patterns (PAMPs) and pro-inflammatory cytokines is dependent on IKKgamma/NEMO and on IKKbeta
additional information
gene disruption via homologous recombination reveals that activation of NF-kappaB in response to pathogen associated molecular patterns (PAMPs) and pro-inflammatory cytokines is dependent on IKKgamma/NEMO and on IKKbeta
additional information
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gene disruption via homologous recombination reveals that activation of NF-kappaB in response to pathogen associated molecular patterns (PAMPs) and pro-inflammatory cytokines is dependent on IKKgamma/NEMO and on IKKbeta
additional information
gene disruption via homologous recombination reveals that IKKalpha, but not IKKbeta, kinase activity is required for activation of an alternative NF-kappaB signaling pathway based on processing of NF-kappaB2/p100:RelB complexes to NF-kappaB2/p52:RelB dimers. In addition, IKKalpha, and not IKKbeta, is required for differentiation of stratified epithelia, such as the epidermis, but this function does not require its protein kinase activity
additional information
gene disruption via homologous recombination reveals that IKKalpha, but not IKKbeta, kinase activity is required for activation of an alternative NF-kappaB signaling pathway based on processing of NF-kappaB2/p100:RelB complexes to NF-kappaB2/p52:RelB dimers. In addition, IKKalpha, and not IKKbeta, is required for differentiation of stratified epithelia, such as the epidermis, but this function does not require its protein kinase activity
additional information
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gene disruption via homologous recombination reveals that IKKalpha, but not IKKbeta, kinase activity is required for activation of an alternative NF-kappaB signaling pathway based on processing of NF-kappaB2/p100:RelB complexes to NF-kappaB2/p52:RelB dimers. In addition, IKKalpha, and not IKKbeta, is required for differentiation of stratified epithelia, such as the epidermis, but this function does not require its protein kinase activity
additional information
Ikkalpha knockin mice are generated in which the two serine phosphoacceptor sites responsible for kinase activation are replaced with alanines. These mice express normal amounts of an IKKalpha protein whose kinase activity cannot be turned on in response to upstream stimuli. TRAMP mice, a mouse model for prostate carcinoma, that are rendered homozygous for the Ikkalpha knockin mutation are found to exhibit decelerated tumor development but eventually all died of primary prostate carcinoma. Knockin mice are found to display much fewer secondary site metastases than wild-type/TRAMP mice, indicating that IKK alpha is an enhancer for prostate metastasis
additional information
Ikkalpha knockin mice are generated in which the two serine phosphoacceptor sites responsible for kinase activation are replaced with alanines. These mice express normal amounts of an IKKalpha protein whose kinase activity cannot be turned on in response to upstream stimuli. TRAMP mice, a mouse model for prostate carcinoma, that are rendered homozygous for the Ikkalpha knockin mutation are found to exhibit decelerated tumor development but eventually all died of primary prostate carcinoma. Knockin mice are found to display much fewer secondary site metastases than wild-type/TRAMP mice, indicating that IKK alpha is an enhancer for prostate metastasis
additional information
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Ikkalpha knockin mice are generated in which the two serine phosphoacceptor sites responsible for kinase activation are replaced with alanines. These mice express normal amounts of an IKKalpha protein whose kinase activity cannot be turned on in response to upstream stimuli. TRAMP mice, a mouse model for prostate carcinoma, that are rendered homozygous for the Ikkalpha knockin mutation are found to exhibit decelerated tumor development but eventually all died of primary prostate carcinoma. Knockin mice are found to display much fewer secondary site metastases than wild-type/TRAMP mice, indicating that IKK alpha is an enhancer for prostate metastasis
additional information
IKKbeta knock-out mice are embryonically lethal
additional information
increased expression of IKKalpha in mouse tumorigenic epidermal cells (PDVC57) leads to changes in the differentiation pattern of the resulting squamous cell carcinomas, originating a distinct histological variant that resembles the human acantholytic squamous cell carcinomas (ASCC) variant
additional information
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increased expression of IKKalpha in mouse tumorigenic epidermal cells (PDVC57) leads to changes in the differentiation pattern of the resulting squamous cell carcinomas, originating a distinct histological variant that resembles the human acantholytic squamous cell carcinomas (ASCC) variant
additional information
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knock-out mice are generated lacking IKK1, IKK2, NEMO(IKKgamma), or both IKK1 and IKK2 in liver parenchymal cells: IKK1 and IKK2 ablation, sensitizes the liver to in vivo LPS challenge, uncovering a redundant function of the two IkappaB kinases in mediating canonical NF-kappaB signaling in hepatocytes and protecting the liver from TNF-induced failure. Knock out mice with combined ablation of IKK1 and IKK2 or IKK1 and NEMO spontaneously develop severe jaundice and fatal cholangitis characterized by inflammatory destruction of small portal bile ducts
additional information
mice lacking the beta subunit of IKK in myeloid cells are more susceptible to endotoxin shock than control mice, which might be a serious challenge for long-term IKKbeta inhibition
additional information
mice lacking the IKKbeta gene in hepatocytes surprisingly show many more and faster growing chemically-induced hepatocellular carcinoma, indicating that in hepatocytes IKKbeta inhibits chemically-induced hepatocellular carcinoma
additional information
mice lacking the IKKbeta gene in hepatocytes surprisingly show many more and faster growing chemically-induced hepatocellular carcinoma, indicating that in hepatocytes IKKbeta inhibits chemically-induced hepatocellular carcinoma
additional information
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mice lacking the IKKbeta gene in hepatocytes surprisingly show many more and faster growing chemically-induced hepatocellular carcinoma, indicating that in hepatocytes IKKbeta inhibits chemically-induced hepatocellular carcinoma
additional information
targeted gene disruption of IKKbeta in intestinal epithelial cells leads to a 80% decline of colitis-associated cancer (CAC) induced by azoxymethane or dextran sulfate sodium salt administration
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targeted gene disruption of IKKbeta in intestinal epithelial cells leads to a 80% decline of colitis-associated cancer (CAC) induced by azoxymethane or dextran sulfate sodium salt administration
additional information
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targeted gene disruption of IKKbeta in intestinal epithelial cells leads to a 80% decline of colitis-associated cancer (CAC) induced by azoxymethane or dextran sulfate sodium salt administration
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targeted gene disruption of IKKbeta in mature macrophages and neutrophils leads to a 50% decrease of tumor multiplicity of colitis-associated cancer (CAC) induced by azoxymethane or dextran sulfate sodium salt administration
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targeted gene disruption of IKKbeta in mature macrophages and neutrophils leads to a 50% decrease of tumor multiplicity of colitis-associated cancer (CAC) induced by azoxymethane or dextran sulfate sodium salt administration
additional information
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targeted gene disruption of IKKbeta in mature macrophages and neutrophils leads to a 50% decrease of tumor multiplicity of colitis-associated cancer (CAC) induced by azoxymethane or dextran sulfate sodium salt administration
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using IKKbeta MCF7 knockout cells it is shown that in MCF7 cells TNF does not activate Akt and requires IKKbeta to activate mTOR
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using TBK1-deficient mice it is shown by bone-marrow transfer experiments that TBK1-mediated signalling in haematopoietic cells is critical for the induction of antigen-specific B and CD41 T cells, whereas in non-haematopoietic cells TBK1 is required for CD81 T-cell induction
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using TBK1-deficient mice it is shown that TBK1 mediates the adjuvant effect of DNA vaccines and is essential for its immunogenicity in mice. Plasmid-DNA-activated, TBK1-dependent signalling and the resultant type-I interferon receptor-mediated signalling is required for induction of antigen-specific B and T cells, which occurred even in the absence of innate immune signalling through a well known CpG DNA sensorToll-like receptor 9 (TLR9) or Z-DNA binding protein 1
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generation of knock-in mice that express a mutant form of IKKalpha that cannot be activated, i.e. IKKalphaAA
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disruption of the gene encoding IKKbeta leads to apoptotic tissue damage, e.g. in mucosa, and prevention of systemic inflammatory response, which results in the multiple organ dysfunction syndrome MODS
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