Information on EC 2.7.11.10 - IkappaB kinase

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The expected taxonomic range for this enzyme is: Eukaryota, Bacteria

EC NUMBER
COMMENTARY hide
2.7.11.10
-
RECOMMENDED NAME
GeneOntology No.
IkappaB kinase
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
ATP + [IkappaB protein] = ADP + [IkappaB phosphoprotein]
show the reaction diagram
ATP + [IkB protein] = ADP + [IkB phosphoprotein]
show the reaction diagram
-
-
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phospho group transfer
SYSTEMATIC NAME
IUBMB Comments
ATP:[IkappaB protein] phosphotransferase
The enzyme phosphorylates IkappaB proteins at specific serine residues, which marks them for destruction via the ubiquitination pathway. Subsequent degradation of the IkB complex (IKK) activates NF-kappaB, a translation factor that plays an important role in inflammation, immunity, cell proliferation and apoptosis. If the serine residues are replaced by threonine residues, the activity of the enzyme is decreased considerably.
CAS REGISTRY NUMBER
COMMENTARY hide
159606-08-3
-
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
Mus musculus BALB/c
Balb/c mice
-
-
Manually annotated by BRENDA team
Mus musculus C57BI/6J
C57BI/6J mice
-
-
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
RH strain in mouse embryonic fibroblast host MEF cells, wild-type and IKKalpha- or IKKbeta-deficient host cells
-
-
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
metabolism
physiological function
additional information
-
homology molecular model of the IKK-2 kinase domain, overview
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
ATP + Bcl
ADP + phosphorylated Bcl
show the reaction diagram
ATP + Bcl
ADP + phosphorylated Bcl10
show the reaction diagram
-
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
show the reaction diagram
-
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
show the reaction diagram
-
activity assay
-
-
?
ATP + IkappaB alpha
ADP + phosphorylated IkappaB alpha
show the reaction diagram
-
-
-
-
?
ATP + IkappaB protein
ADP + IkappaB phosphoprotein
show the reaction diagram
-
-
-
-
?
ATP + IkappaB protein
ADP + phosphorylated IkappaB
show the reaction diagram
-
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
show the reaction diagram
ATP + IkappaBalpha
ADP + phosphorylated-IkappaBalpha
show the reaction diagram
-
-
-
-
?
ATP + IkappaBbeta
ADP + phosphorylated IkappaBbeta
show the reaction diagram
-
phosphorylation of IkappaBalpha at Ser19 and Ser23
-
-
?
ATP + interferon regulatory factor 3
ADP + phosphorylated interferon regulatory factor 3
show the reaction diagram
-
-
-
-
?
ATP + KKKKERLLDDRHDSGLDSMKDEE
ADP + phosphorylated-KKKKERLLDDRHDSGLDSMKDEE
show the reaction diagram
-
IKK substrate peptide derived from IkappaBalpha sequence
-
-
?
ATP + NF-kappaB p65 subunit
ADP + phosphorylated NF-kappaB p65 subunit
show the reaction diagram
-
IKKalpha and IKKbeta phosphorylate NF-kappaB p65 subunit at Ser536
-
-
?
ATP + p65/RelA
ADP + phosphorylated p65/RelA
show the reaction diagram
-
-
-
-
?
ATP + protein p100
ADP + phosphorylated protein p100
show the reaction diagram
ATP + protein p165
ADP + phosphorylated protein p165
show the reaction diagram
ATP + STAT1 transcription factor
ADP + phosphorylated STAT1 transcription factor
show the reaction diagram
-
-
-
-
?
ATP + [acetylated histone H3 protein]
ADP + [acetylated histone H3 phosphoprotein]
show the reaction diagram
ATP + [biotinylated IkappaBa peptide]
ADP + [biotinylated IkappaBa phosphopeptide]
show the reaction diagram
-
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]
show the reaction diagram
-
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]
show the reaction diagram
-
-
-
-
?
ATP + [GST-IkappaBalpha protein]
ADP + [GST-IkappaBalpha phosphoprotein]
show the reaction diagram
-
-
-
-
?
ATP + [GST-IkappaBalpha1-54 protein]
ADP + [GST-IkappaBalpha1-54 phosphoprotein]
show the reaction diagram
ATP + [GST-IkappaBbeta protein]
ADP + [GST-IkappaBbeta phosphoprotein]
show the reaction diagram
-
-
-
-
?
ATP + [histone H3 protein]
ADP + [histone H3 phosphoprotein]
show the reaction diagram
ATP + [IFN regulatory factor 3 protein (380-427)]
ADP + [IFN regulatory factor 3 phosphoprotein (380-427)]
show the reaction diagram
-
the truncated mutant is a good substrate
-
-
?
ATP + [IFN regulatory factor 3 protein]
ADP + [IFN regulatory factor 3 phosphoprotein]
show the reaction diagram
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
show the reaction diagram
ATP + [IkappaBalpha protein]
ADP + [IkappaBalpha phosphoprotein]
show the reaction diagram
ATP + [IkappaBbeta protein]
ADP + [IkappaBbeta phosphoprotein]
show the reaction diagram
ATP + [IRF3 protein]
ADP + [IRF3 phosphoprotein]
show the reaction diagram
-
phosphorylation at Ser396 by IKK-related IKKepsilon and TBK1 kinase
-
-
?
ATP + [leucine-rich repeat kinase 2 protein]
ADP + [leucine-rich repeat kinase 2 phosphoprotein]
show the reaction diagram
ATP + [NFkappaB subunit p56]
ADP + [NFkappaB subunit p56]phosphate
show the reaction diagram
ATP + [optineurin protein]
ADP + [optineurin phosphoprotein]
show the reaction diagram
-
phosphorylation at Ser177 by IKK-related IKKepsilon and TBK1 kinase
-
-
?
ATP + [p73 protein]
ADP + [p73 phosphoprotein]
show the reaction diagram
-
IKKalpha in the nucleus
-
-
?
ATP + [RelA/p65 protein]
ADP + [RelA/p65 phosphoprotein]
show the reaction diagram
ATP + [S386A IFN regulatory factor 3 protein]
ADP + [S386A IFN regulatory factor 3 phosphoprotein]
show the reaction diagram
-
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]
show the reaction diagram
-
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]
show the reaction diagram
-
low activity with the IRF3 mutant
-
-
?
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
ATP + Bcl
ADP + phosphorylated Bcl
show the reaction diagram
ATP + Bcl10
ADP + phosphorylated Bcl10
show the reaction diagram
-
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
show the reaction diagram
-
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
show the reaction diagram
ATP + protein p100
ADP + phosphorylated protein p100
show the reaction diagram
-
interaction with the NF-kappaB complex
-
-
?
ATP + protein p165
ADP + phosphorylated protein p165
show the reaction diagram
-
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]
show the reaction diagram
ATP + [GST-IkappaB protein]
ADP + [GST-IkappaB phosphoprotein]
show the reaction diagram
-
-
-
-
?
ATP + [GST-IkappaBalpha protein]
ADP + [GST-IkappaBalpha phosphoprotein]
show the reaction diagram
-
-
-
-
?
ATP + [histone H3 protein]
ADP + [histone H3 phosphoprotein]
show the reaction diagram
ATP + [IFN regulatory factor 3 protein]
ADP + [IFN regulatory factor 3 phosphoprotein]
show the reaction diagram
-
IRF3 activation is triggered by IKKepsilon/TBK1-mediated phosphorylation on Ser396
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
show the reaction diagram
ATP + [IkappaBalpha protein]
ADP + [IkappaBalpha phosphoprotein]
show the reaction diagram
ATP + [IkappaBbeta protein]
ADP + [IkappaBbeta phosphoprotein]
show the reaction diagram
-
-
-
-
?
ATP + [IRF3 protein]
ADP + [IRF3 phosphoprotein]
show the reaction diagram
-
phosphorylation at Ser396 by IKK-related IKKepsilon and TBK1 kinase
-
-
?
ATP + [leucine-rich repeat kinase 2 protein]
ADP + [leucine-rich repeat kinase 2 phosphoprotein]
show the reaction diagram
-
catalyzed reaction of canonical IKKalpha and IKKbeta and IKK-related IKKepsilon and TBK1 kinase
-
-
?
ATP + [NFkappaB subunit p56]
ADP + [NFkappaB subunit p56]phosphate
show the reaction diagram
-
-
-
-
?
ATP + [optineurin protein]
ADP + [optineurin phosphoprotein]
show the reaction diagram
-
phosphorylation at Ser177 by IKK-related IKKepsilon and TBK1 kinase
-
-
?
ATP + [p73 protein]
ADP + [p73 phosphoprotein]
show the reaction diagram
-
IKKalpha in the nucleus
-
-
?
ATP + [RelA/p65 protein]
ADP + [RelA/p65 phosphoprotein]
show the reaction diagram
-
-
-
-
?
additional information
?
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Mn2+
-
-
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)phenyl)acetic acid
-
IC50 for the IKKbeta is 0.0022 mM
(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
-
-
(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
-
-
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-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanamine
-
-
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-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-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
-
-
2-methanesulfonyl-4-methyl-7-methylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
-
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
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
-
-
3-amino-4-(1-benzofuran-2-yl)-6-methylthieno[2,3-b]pyridine-2-carboxamide
-
-
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
-
-
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-(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-(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-(7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]isoquinolin-6-yl)benzenesulfonamide
-
-
4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzoic acid
-
IC50 for the IKK complex is 0.018 mM, cellular profile
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-[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
-
-
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
6,8-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-(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
Acetylsalicylic acid
antirheumatic gold compound
-
inhibition of IKKbeta
-
arsenic trioxide
arsenite
-
inhibition of IKKbeta
AS602868
Bay 11-7082
-
-
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
BX795
-
-
-
chalcone
-
-
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
IMD-0354
LY294002
-
phosphorylation of IKKalphaT23 is inhibited both by LY294002 and wortmannin, but phosphorylation of Ser176/Ser180 is not
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-(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
-
-
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
noraristeromycin
-
NAM
PHA-408
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
salicylate
-
weak inhibition of IKK-2
shRNA
-
-
-
sulfasalazine
sulindac sulfide
tetrandrine
-
a bis-benzylisoquinoline alkaloid isolated from the roots of Han-Fang-Ji (Stephania Tetrandra S Moore) effectively inhibits IKKs phosphorylation
trans-resveratrol
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
-
additional information
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
alloferon
-
alloferon, a 13-amino acid peptide isolated from the bacteria-challenged larvae of the blow fly Calliphora vicina, activates IKK activity
CD28
-
activates Vav-1/IKKalpha and subsequently NFkappaB, meditated by Vav-1
-
cdc37
-
the chaperone protein associates with the IKK complex and is required for its TNFalpha-induced activation
-
glycogen synthase kinase-3beta
-
GSK-3 is required for constitutive IKK activity; GSK-3 is required for constitutive IKK activity
-
HSP70
-
the chaperone protein associates with the IKK complex and is required for its TNFalpha-induced activation
-
Hsp90
-
the chaperone protein associates with the IKK complex and is required for its TNFalpha-induced activation
-
human leukemia virus type-1 TAX
-
TAX is binding to and activating the IKK complex. A sustained activation of the Tax-mediated activation of the NFkappaB pathway is dependent on an intact Hsp90-IKK complex
-
mTOR
-
mTOR (mammalian target of rapamycin) controls phosphorylation of IkappaBalpha and p65/RelA as shown by knockdown of mTOR in PC3 cells. Furthermore, overexpression of mTOR stimulates IKK activity; mTOR (mammalian target of rapamycin) controls phosphorylation of IkappaBalpha and p65/RelA as shown by knockdown of mTOR in PC3 cells. Furthermore, overexpression of mTOR stimulates IKK activity
-
raptor
-
raptor (mTOR associated protein) controls phosphorylation of IkappaBalpha and p65/RelA as shown by knockdown of raptor in PC3 cells; raptor (mTOR associated protein) controls phosphorylation of IkappaBalpha and p65/RelA as shown by knockdown of raptor in PC3 cells
-
TAK1
-
critical direct upsteam activating kinase of IKK
-
Tax
-
viral oncoprotein, activates by direct binding, involved in ubiquitination and phosphorylation
-
TNF-alpha
-
-
-
TNFalpha
TRAF6
-
upstream activator of IKK kinase complex
-
tumor necrosis factor TNFalpha
Vav-1
-
cytoplasmic proto-oncogene, constitutively associates with IKKalpha in Jurkat and primary CD4+ cells
-
additional information
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
additional information
additional information
-
kinetics of IkappaB phosphorylation by parasite IKK, host NF-kappaB activation reveals a biphasic, hierarchical, and temporally regulated response
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000006
8-(5-chloro-2-(4-methylpiperazin-1-yl)isonicotinamido)-1-(4-fluorophenyl)-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide
-
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
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
0.00052 - 0.0043
1,4-dimethyl-7-methylamino-2-phenyl-4H-imidazo[4,5-d]imidazo[5,4-b]pyridine
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
-
-
0.000056 - 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
0.000025
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
0.001
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
0.00025
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
0.0008
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
0.001 - 0.0251
4-(7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]isoquinolin-6-yl)benzenesulfonamide
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
0.00013
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
0.0126
4-[7-(piperidin-3-yloxy)isoquinolin-6-yl]benzenesulfonamide
Homo sapiens
-
IKK-alpha
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
0.0006
5,6-dibromo-beta-carboline
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]
0.0007
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
0.003
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
-
-
0.00037 - 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
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT <