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Information on EC 2.7.11.10 - IkappaB kinase and Organism(s) Homo sapiens and UniProt Accession Q14164

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     2 Transferases
         2.7 Transferring phosphorus-containing groups
             2.7.11 Protein-serine/threonine kinases
                2.7.11.10 IkappaB kinase
IUBMB Comments
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.
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Homo sapiens
UNIPROT: Q14164
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Word Map
The taxonomic range for the selected organisms is: Homo sapiens
The expected taxonomic range for this enzyme is: Eukaryota, Bacteria
Synonyms
ikappabalpha, ikkbeta, ikappab kinase, ikkalpha, ikk complex, lrrk2 kinase, tank-binding kinase 1, ikk-beta, ikkepsilon, ikk-2, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
I-kappa-B kinase epsilon
-
IkappaB kinase epsilon
-
IKKepsilon
-
inhibitor of nuclear factor kappa-B kinase epsilon subunit
-
CHUK
-
-
I kappa B kinase alpha
-
-
I-kappa B kinase epsilon
-
-
Ikappa B kinase alpha
-
-
IkappaB alpha kinase
-
IkappaB kinase alpha
IkappaB kinase beta
IkappaB kinase complex
-
-
IkappaB kinase-1
-
IkappaB kinase-2
-
IkappaB kinase-beta
-
-
IkappaBalpha
-
IkappaBalpha kinase
-
-
IkappaBbeta kinase
-
-
IKK complex
-
-
IKK-beta
IKKalpha
IKKbeta
IKKepsilon
-
-
inhibitor kappa-B kinase-beta
-
inhibitor of kappaB kinase
-
-
inhibitor of nuclear factor kappa B kinase beta subunit inhibitor of nuclear factor kappa-B kinase alpha subunit
inhibitory kappa B kinase alpha
-
inhibitory kappa B kinase beta
-
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
ATP + [IkappaB protein] = ADP + [IkappaB phosphoprotein]
show the reaction diagram
activation and reaction mechanism
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phospho group transfer
-
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
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ATP + interferon regulatory factor 3
ADP + phosphorylated interferon regulatory factor 3
show the reaction diagram
-
-
-
?
ATP + STAT1 transcription factor
ADP + phosphorylated STAT1 transcription factor
show the reaction diagram
-
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
show the reaction diagram
-
-
-
?
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 + IkappaBalpha
ADP + phosphorylated IkappaBalpha
show the reaction diagram
ATP + KKKKERLLDDRHDSGLDSMKDEE
ADP + phosphorylated-KKKKERLLDDRHDSGLDSMKDEE
show the reaction diagram
-
IKK substrate peptide derived from IkappaBalpha sequence
-
-
?
ATP + NF-kappaB
ADP + phosphorylated NF-kappaB
show the reaction diagram
-
-
-
-
?
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 + [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 + [histone H3 protein]
ADP + [histone H3 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 + [NFkappaB subunit p56]
ADP + [NFkappaB subunit p56]phosphate
show the reaction diagram
ATP + [p73 protein]
ADP + [p73 phosphoprotein]
show the reaction diagram
-
IKKalpha in the nucleus
-
-
?
additional information
?
-
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
show the reaction diagram
-
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
ATP + Bcl
ADP + phosphorylated Bcl
show the reaction diagram
-
phosphorylation at the C-terminus of Bcl by IKKbeta disrupts Bcl10/Malt1 association and Bcl10-mediated signaling
-
-
?
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 + IkappaBalpha
ADP + phosphorylated IkappaBalpha
show the reaction diagram
ATP + NF-kappaB
ADP + phosphorylated NF-kappaB
show the reaction diagram
-
-
-
-
?
ATP + [acetylated histone H3 protein]
ADP + [acetylated histone H3 phosphoprotein]
show the reaction diagram
-
IKKalpha is required for histone function regulation in the nucleus
-
-
?
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 + [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 + [NFkappaB subunit p56]
ADP + [NFkappaB subunit p56]phosphate
show the reaction diagram
-
-
-
-
?
ATP + [p73 protein]
ADP + [p73 phosphoprotein]
show the reaction diagram
-
IKKalpha in the nucleus
-
-
?
additional information
?
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Mn2+
-
-
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
chrysin
chrysin interacts weakly with the I-kappa-B kinase epsilon binding site and inhibits the enzyme at doses higher than 0.06 mM
(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
-
(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
-
-
1088 P protein
-
-
-
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
-
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
-
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
-
2-amino-4-(benzylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
-
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
-
2-amino-4-(cyclohexylmethylamino)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
-
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
-
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
-
BMS-066, inhibitor of IKKbeta
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
-
3-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-benzenesulfonamide
-
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-((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
-
BMS-345541, inhibitor of IKKbeta
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
PHA-408, ATP-competitive, selective IKK-2 inhibitor
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
-
nonspecific for IKK, anti-inflammatory
antirheumatic gold compound
-
inhibition of IKKbeta
-
arsenic trioxide
-
nonspecific for IKK, acts on a cystein ersidue in the activation loop
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
BMS-345541
-
specific for IKK-2, binds at an allosteric site
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
-
specific IKKbeta inhibition
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
-
-
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
-
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
a selective IKK-2 inhibitor, shows time-dependent binding to the enzyme
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
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
-
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
-
salicylate
-
weak inhibition of IKK-2
shRNA
-
-
-
sulfasalazine
sulindac sulfide
-
nonspecific for IKK, anti-inflammatory
trans-resveratrol
-
nonspecific for IKK, anti-inflammatory
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
-
glycogen synthase kinase-3beta
GSK-3 is required for constitutive IKK activity
-
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
-
NEMO
-
raptor
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
-
and other cytokines, activation of IKK activating NF-kappaB
-
TRAF6
-
upstream activator of IKK kinase complex
-
tumor necrosis factor TNFalpha
-
cytokines activate the IKK complex, mechanism, overview
-
Vav-1
-
cytoplasmic proto-oncogene, constitutively associates with IKKalpha in Jurkat and primary CD4+ cells
-
additional information
-
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
0.000041
BX795
Homo sapiens
-
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]
0.007
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
0.0001
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
-
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
22
-
activity assay at room temperature
additional information
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
cell line KG-1
Manually annotated by BRENDA team
-
chronically infected with HIV-1
Manually annotated by BRENDA team
-
bronchial epithelial cell line
Manually annotated by BRENDA team
-
colon cancer cell line
Manually annotated by BRENDA team
-
colon cancer cell line
Manually annotated by BRENDA team
-
from umbilical vein
Manually annotated by BRENDA team
-
chronically infected with HIV-1
Manually annotated by BRENDA team
-
primary
Manually annotated by BRENDA team
-
epidermal
Manually annotated by BRENDA team
-
respiratory tract mucosa
Manually annotated by BRENDA team
-
primary
Manually annotated by BRENDA team
-
mycosis fungoides cell line
Manually annotated by BRENDA team
-
lung adenocarcinoma cell line
Manually annotated by BRENDA team
in human acantholytic squamous cell carcinoma IKKalpha and E-cadherin are strongly expressed, with absence of keratins K1 and K10, usually co-expressed with IKKalpha and E-cadherin
Manually annotated by BRENDA team
additional information
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
in T-cells
Manually annotated by BRENDA team
additional information
-
treatment with ATM inhibitors blocks the nuclear IKKalpha accumulation by cisplatin, suggesting that ATM plays a role in the nuclear translocation of IKKalpha
-
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
physiological function
the enzyme is responsible for production of pro inflammatory cytokine and suppression of energy expenditure genes, finally causing insulin resistance and obesity
malfunction
-
suppression of NF-betaB activation by nimbolide is caused by inhibition of IkappaB kinase, which leads to suppression of IkappaBalpha phosphorylation and degradation, nuclear translocation, DNA binding, and gene transcription. Nimbolide suppresses TNF-alpha-induced tumor cell invasion and NF-kappaB activation in a not-cell-specific manner
metabolism
physiological function
additional information
homology molecular model of the IKK-2 kinase domain, overview
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
IKKE_HUMAN
716
0
80462
Swiss-Prot
other Location (Reliability: 2)
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
700000
-
IKK complex
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
dimer
heterotrimer
oligomer
additional information
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phosphoprotein
additional information
-
within its activation loop, IKKbeta contains an evolutionarily conserved LxxLAP consensus motif for hydroxylation by prolyl hydroxylases
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
C179A
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
S177E/S181E
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
additional information
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
cytoplasmic extracts are prepared
-
native IkappaBalpha kinase from HeLa S3 cells by ammonium sulfate fractionation, ultrafiltration, and gel filtration
-
nuclear and cytoplasmic extracts are prepared
-
recombinant C-terminally FLAG-tagged wild-type and mutant IKK-2s
recombinant GST-fusion IKKgamma protein from Escherichia coli strain BL21 by glutathione affinity and anion exchange chromatography, and gel filtration, recombinant His-tagged IKKgamma protein from Escherichia coli strain BL21 by nickel affinity chromatography
-
recombinant His-tagged IKKbeta from Sf21 insect cells by nickel affinity chromatography
-
using Ni-NTA-chromatography
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
into the vector pSC-b for sequencing, subsequently into pCMV-FLAG-1 or pEBG6P
a Flag-tagged IKKbeta expression vector is used
-
a GST-IkappaBalpha fusion protein is generated
coexpression of FLAG-atgged wild-type and mutant IKKbeta proteins with T7-tagged IKKgamma and HA-tagged ubiquitin in 293T cells
-
coexpression of FLAG-tagged IKKbeta, T7-tagged IKKgamma, and Tax in 293T cells and in murine embryonic fibroblasts devoid of the enzyme
-
coexpression of HA-tagged IKKbeta and GST-fusion IKKgamma in 293 cells, expression of GST-fusion or His-tagged IKKgamma protein in Escherichia coli strain BL21
-
coexpression of Myc-tagged NEMO/IKKgamma, FLAG-tagged p65, and HA-tagged or GST-tagged CREB-binding protein in 293T cells or in mouse embryonic fibroblasts MEF cell line
-
expressed in baculovirus-infected Sf9 cells
expressed in baculovirus-infected sf9 insect cells
expressed in Escherichia coli as a His-tagged fusion protein
expression of C-terminally FLAG-tagged wild-type and mutant IKK-2s
expression of FLAG- or HA-tagged wild-type and mutant IKKbeta in HEK-293 and HeLa cells
-
expression of GST-tagged IKKalpha and IKKbeta in HEK-293 cells, coexpression of IKKbeta and GFP-tagged DELTANp73alpha protein in HEK-293 cells
-
expression of mutant IKKbeta and IKKalpha in HeLa cells and in HEK293 cells, expression of His-tagged IKKbeta in Spodoptera frugiperda Sf21 cells via baculovirus infection
-
expression of Myc-tagged IKK-alpha or IKK-beta in mouse embryonic fibroblasts MEF cell line
-
expression of wild-type FLAG-tagged IKK-beta or FLAG-tagged IKK-beta mutant C179A in A-293 cells
-
Flag-IKKalpha and Flag-IKKbeta vectors for transfection of HEK293 cells are used
-
IKKalpha, IKKbeta and IKKgamma, cloned into pRK-FLAG or pRK-HA, are used, IKKbeta fragments, aa1-398, aa399-576, aa577-756, are inserted into the vector pRK-FLAG
-
recombinant human IKK-beta, residues 1-737, is expressed in Baculovirus as a C-terminal GST-tagged fusion protein, a 6-His-tagged full length IKK-alpha construct is used
-
transient coexpression of IKKepsilon, IRF3, and TBK1 or IKKbeta in 293T cells, transient coexpression of IFN-beta or ISRE reporter genes and IKKepsilon or TBK1 in HEK293 cells with or without FLAG or GFP tag
-
transient expression of HA-tagged IKKalpha, IKKbeta, and IKKalpha mutant L605R/F606P in Jurkat cells, transient coexpression of myc-tagged Vav-1 and IKKalpha in Jurkat cells
-
transient expression of wild-type and mutant FLAG-tagged IKK2 in HELF cells
-
transient expression of wild-type and mutant IKKbeta in HeLa cells
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
I-kappa-B kinase epsilon expression is induced by polyinosinic-polycytidylic acid
IKKalpha and IKKbeta downregulation in 38E6E7HFK cells by siRNA expression
-
the enzyme is underexpressed in highly invasive SUNE-1-5-8F cells compared with non-invasive cells (SUNE-1 and SUNE-6-10B)
-
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
drug development
because of its central role in the overall NF-kappaB regulation, IKK-2 is a viable target for drug discovery
medicine
molecular biology
pharmacology
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Hu, M.C.; Wang, Y.
IkappaB kinase-alpha and -beta genes are coexpressed in adult and embryonic tissues but localized to different human chromosomes
Gene
222
31-40
1998
Homo sapiens (O14920), Homo sapiens (O15111), Homo sapiens
Manually annotated by BRENDA team
Jobin, C.; Sartor, R.B.
The I kappa B/NF-kappa B system: a key determinant of mucosalinflammation and protection
Am. J. Physiol.
278
C451-462
2000
Homo sapiens (O14920), Homo sapiens (O15111), Mus musculus (O88351), Mus musculus (Q60680), Rattus norvegicus (Q9QY78)
Manually annotated by BRENDA team
Mercurio, F.; Zhu, H.; Murray, B.W.; Shevchenko, A.; Bennett, B.L.; Li, J.; Young, D.B.; Barbosa, M.; Mann, M.; Manning, A.; Rao, A.
IKK-1 and IKK-2: cytokine-activated IkappaB kinases essential for NF-kappaB activation
Science
278
860-866
1997
Homo sapiens (O14920), Homo sapiens (O15111)
Manually annotated by BRENDA team
Nemoto, S.; DiDonato, J.A.; Lin, A.
Coordinate regulation of IkappaB kinases by mitogen-activated protein kinase kinase kinase 1 and NF-kappaB-inducing kinase
Mol. Cell. Biol.
18
7336-7343
1998
Homo sapiens (O14920), Homo sapiens (O15111), Mus musculus (O88351), Mus musculus (Q60680), Rattus norvegicus (Q9QY78)
Manually annotated by BRENDA team
Shindo, M.; Nakano, H.; Sakon, S.; Yagita, H.; Mihara, M.; Okumura, K.
Assignment of IkappaB kinase beta (IKBKB) to human chromosome band 8p12->p11 by in situ hybridization
Cytogenet. Cell Genet.
82
32-33
1998
Homo sapiens (O14920), Homo sapiens
Manually annotated by BRENDA team
Woronicz, J.D.; Gao, X.; Cao, Z.; Rothe, M.; Goeddel, D.V.
IkappaB kinase-beta: NF-kappaB activation and complex formation with IkappaB kinase-alpha and NIK
Science
278
866-869
1997
Homo sapiens (O14920)
Manually annotated by BRENDA team
Wu, R.C.; Qin, J.; Hashimoto, Y.; Wong, J.; Xu, J.; Tsai, S.Y.; Tsai, M.J.; O'Malley, B.W.
Regulation of SRC-3 (pCIP/ACTR/AIB-1/RAC-3/TRAM-1) Coactivator activity by I kappa B kinase
Mol. Cell. Biol.
22
3549-3561
2002
Homo sapiens (O14920)
Manually annotated by BRENDA team
Connelly, M.A.; Marcu, K.B.
CHUK, a new member of the helix-loop-helix and leucine zipper families of interacting proteins, contains a serine-threonine kinase catalytic domain
Cell. Mol. Biol. Res.
41
537-549
1995
Homo sapiens (O15111), Mus musculus (Q60680)
Manually annotated by BRENDA team
Delhase, M.; Hayakawa, M.; Chen, Y.; Karin, M.
Positive and negative regulation of IkappaB kinase activity through IKKbeta subunit phosphorylation
Science
284
309-313
1999
Homo sapiens (O15111), Mus musculus (Q60680)
Manually annotated by BRENDA team
DiDonato, J.A.; Hayakawa, M.; Rothwarf, D.M.; Zandi, E.; Karin, M.
A cytokine-responsive IkappaB kinase that activates the transcription factor NF-kappaB
Nature
388
548-554
1997
Homo sapiens (O15111)
Manually annotated by BRENDA team
Ling, L.; Cao, Z.; Goeddel, D.V.
NF-kappaB-inducing kinase activates IKK-alpha by phosphorylation of Ser-176
Proc. Natl. Acad. Sci. USA
95
3792-3797
1998
Homo sapiens (O15111)
Manually annotated by BRENDA team
Ozes, O.N.; Mayo, L.D.; Gustin, J.A.; Pfeffer, S.R.; Pfeffer, L.M.; Donner, D.B.
NF-kappaB activation by tumour necrosis factor requires the Akt serine-threonine kinase
Nature
401
82-85
1999
Homo sapiens (O15111)
Manually annotated by BRENDA team
Regnier, C.H.; Song, H.Y.; Gao, X.; Goeddel, D.V.; Cao, Z.; Rothe, M.
Identification and characterization of an IkappaB kinase
Cell
90
373-383
1997
Homo sapiens (O15111)
Manually annotated by BRENDA team
Nagase, T.; Seki, N.; Tanaka, A.; Ishikawa, K.; Nomura, N.
Prediction of the coding sequences of unidentified human genes. IV. The coding sequences of 40 new genes (KIAA0121-KIAA0160) deduced by analysis of cDNA clones from human cell line KG-1
DNA Res.
2; 167-174
199-210
1995
Homo sapiens (Q14164)
-
Manually annotated by BRENDA team
Peters, R.T.; Liao, S.M.; Maniatis, T.
IKKepsilon is part of a novel PMA-inducible IkappaB kinase complex
Mol. Cell
5
513-522
2000
Homo sapiens (Q14164)
Manually annotated by BRENDA team
Shimada, T.; Kawai, T.; Takeda, K.; Matsumoto, M.; Inoue, J.; Tatsumi, Y.; Kanamaru, A.; Akira, S.
IKK-i, a novel lipopolysaccharide-inducible kinase that is related to IkappaB kinases
Int. Immunol.
11
1357-1362
1999
Homo sapiens (Q14164), Mus musculus (Q9R0T8), Mus musculus
Manually annotated by BRENDA team
Amici, C.; Belardo, G.; Rozera, C.; Bernasconi, D.; Santoro, M.G.
Inhibition of herpesvirus-induced HIV-1 replication by cyclopentenone prostaglandins: role of IkappaB kinase (IKK)
Aids
18
1271-1280
2004
Homo sapiens
Manually annotated by BRENDA team
Castro, A.C.; Dang, L.C.; Soucy, F.; Grenier, L.; Mazdiyasni, H.; Hottelet, M.; Parent, L.; Pien, C.; Palombella, V.; Adams, J.
Novel IKK inhibitors: beta-carbolines
Bioorg. Med. Chem. Lett.
13
2419-2422
2003
Homo sapiens
Manually annotated by BRENDA team
Waelchli, R.; Bollbuck, B.; Bruns, C.; Buhl, T.; Eder, J.; Feifel, R.; Hersperger, R.; Janser, P.; Revesz, L.; Zerwes, H.G.; Schlapbach, A.
Design and preparation of 2-benzamido-pyrimidines as inhibitors of IKK
Bioorg. Med. Chem. Lett.
16
108-112
2006
Homo sapiens
Manually annotated by BRENDA team
Burke, J.R.
Targeting IkB kinase for the treatment of inflammatory and other disorders
Curr. Opin. Drug Discov. Devel.
6
720-728
2003
Homo sapiens
Manually annotated by BRENDA team
Carter, R.S.; Pennington, K.N.; Ungurait, B.J.; Ballard, D.W.
In vivo identification of inducible phosphoacceptors in the IKKgamma/NEMO subunit of human IkappaB kinase
J. Biol. Chem.
278
19642-19648
2003
Homo sapiens
Manually annotated by BRENDA team
Sakurai, H.; Suzuki, S.; Kawasaki, N.; Nakano, H.; Okazaki, T.; Chino, A.; Doi, T.; Saiki, I.
Tumor necrosis factor-alpha-induced IKK phosphorylation of NF-kappaB p65 on serine 536 is mediated through the TRAF2, TRAF5, and TAK1 signaling pathway
J. Biol. Chem.
278
36916-36923
2003
Homo sapiens
Manually annotated by BRENDA team
Tang, E.D.; Wang, C.Y.; Xiong, Y.; Guan, K.L.
A role for NF-kappaB essential modifier/IkappaB kinase-gamma (NEMO/IKKgamma) ubiquitination in the activation of the IkappaB kinase complex by tumor necrosis factor-alpha
J. Biol. Chem.
278
37297-37305
2003
Homo sapiens
Manually annotated by BRENDA team
Verma, U.N.; Yamamoto, Y.; Prajapati, S.; Gaynor, R.B.
Nuclear role of IkappaB kinase-gamma/NF-kappaB essential modulator (IKK gamma/NEMO) in NF-kappaB-dependent gene expression
J. Biol. Chem.
279
3509-3515
2004
Homo sapiens
Manually annotated by BRENDA team
Takada, Y.; Kobayashi, Y.; Aggarwal, B.B.
Evodiamine abolishes constitutive and inducible NF-kB activation by inhibiting IkBalpha kinase Activation, Thereby Suppressing NF-kB-regulated antiapoptotic and metastatic gene expression, up-regulating apoptosis, and inhibiting invasion
J. Biol. Chem.
280
17203-17212
2005
Homo sapiens
Manually annotated by BRENDA team
Carter, R.S.; Pennington, K.N.; Arrate, P.; Oltz, E.M.; Ballard, D.W.
Site-specific monoubiquitination of IkappaB kinase IKKbeta regulates its phosphorylation and persistent activation
J. Biol. Chem.
280
43272-43279
2005
Homo sapiens
Manually annotated by BRENDA team
Wang, L.C.; Okitsu, C.Y.; Zandi, E.
Tumor necrosis factor alpha-dependent drug resistance to purine and pyrimidine analogues in human colon tumor cells mediated through IKK
J. Biol. Chem.
280
7634-7644
2005
Homo sapiens
Manually annotated by BRENDA team
Luo, J.L.; Kamata, H.; Karin, M.
IKK/NF-kappaB signaling: balancing life and death - a new approach to cancer therapy
J. Clin. Invest.
115
2625-2632
2005
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Piccolella, E.; Spadaro, F.; Ramoni, C.; Marinari, B.; Costanzo, A.; Levrero, M.; Thomson, L.; Abraham, R.T.; Tuosto, L.
Vav-1 and the IKKalpha subunit of IkappaB kinase functionally associate to induce NF-kappaB activation in response to CD28 engagement
J. Immunol.
170
2895-2903
2003
Homo sapiens
Manually annotated by BRENDA team
Tegeder, I.; Niederberger, E.; Schmidt, R.; Kunz, S.; Guehring, H.; Ritzeler, O.; Michaelis, M.; Geisslinger, G.
Specific inhibition of IkB kinase reduces hyperalgesia in inflammatory and neuropathic pain models in rats
J. Neurosci.
24
1637-1645
2004
Homo sapiens
Manually annotated by BRENDA team
Caposio, P.; Dreano, M.; Garotta, G.; Gribaudo, G.; Landolfo, S.
Human cytomegalovirus stimulates cellular IKK2 activity and requires the enzyme for productive replication
J. Virol.
78
3190-3195
2004
Homo sapiens
Manually annotated by BRENDA team
Tegethoff, S.; Behlke, J.; Scheidereit, C.
Tetrameric oligomerization of IkappaB kinase gamma (IKKgamma) is obligatory for IKK complex activity and NF-kappaB activation
Mol. Cell. Biol.
23
2029-2041
2003
Homo sapiens
Manually annotated by BRENDA team
Fitzgerald, K.A.; McWhirter, S.M.; Faia, K.L.; Rowe, D.C.; Latz, E.; Golenbock, D.T.; Coyle, A.J.; Liao, S.M.; Maniatis, T.
IKKepsilon and TBK1 are essential components of the IRF3 signaling pathway
Nat. Immunol.
4
491-496
2003
Homo sapiens
Manually annotated by BRENDA team
Yamamoto, Y.; Verma, U.N.; Prajapati, S.; Kwak, Y.T.; Gaynor, R.B.
Histone H3 phosphorylation by IKK-alpha is critical for cytokine-induced gene expression
Nature
423
655-659
2003
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Yamamoto, Y.; Gaynor, R.B.
IkB kinases: key regulators of the NF-kB pathway
Trends Biochem. Sci.
29
72-79
2004
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Byun, M.S.; Choi, J.; Jue, D.M.
Cysteine-179 of IkappaB kinase beta plays a critical role in enzyme activation by promoting phosphorylation of activation loop serines
Exp. Mol. Med.
38
546-552
2006
Homo sapiens
Manually annotated by BRENDA team
Ha, U.; Lim, J.H.; Jono, H.; Koga, T.; Srivastava, A.; Malley, R.; Pages, G.; Pouyssegur, J.; Li, J.D.
A novel role for IkappaB kinase (IKK) alpha and IKKbeta in ERK-dependent up-regulation of MUC5AC mucin transcription by Streptococcus pneumoniae
J. Immunol.
178
1736-1747
2007
Homo sapiens, Mus musculus, Mus musculus BALB/c
Manually annotated by BRENDA team
Ahn, K.S.; Sethi, G.; Aggarwal, B.B.
Simvastatin potentiates TNF-alpha-induced apoptosis through the down-regulation of NF-kappaB-dependent antiapoptotic gene products: role of IkappaBalpha kinase and TGF-beta-activated kinase-1
J. Immunol.
178
2507-2516
2007
Homo sapiens
Manually annotated by BRENDA team
Hansberger, M.W.; Campbell, J.A.; Danthi, P.; Arrate, P.; Pennington, K.N.; Marcu, K.B.; Ballard, D.W.; Dermody, T.S.
IkappaB kinase subunits alpha and gamma are required for activation of NF-kappaB and induction of apoptosis by mammalian reovirus
J. Virol.
81
1360-1371
2007
Homo sapiens
Manually annotated by BRENDA team
Wegener, E.; Oeckinghaus, A.; Papadopoulou, N.; Lavitas, L.; Schmidt-Supprian, M.; Ferch, U.; Mak, T.W.; Ruland, J.; Heissmeyer, V.; Krappmann, D.
Essential role for IkappaB kinase beta in remodeling Carma1-Bcl10-Malt1 complexes upon T cell activation
Mol. Cell
23
13-23
2006
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Edwards, M.R.; Hewson, C.A.; Laza-Stanca, V.; Lau, H.T.; Mukaida, N.; Hershenson, M.B.; Johnston, S.L.
Protein kinase R, IkappaB kinase-beta and NF-kappaB are required for human rhinovirus induced pro-inflammatory cytokine production in bronchial epithelial cells
Mol. Immunol.
44
1587-1597
2007
Homo sapiens
Manually annotated by BRENDA team
Cummins, E.P.; Berra, E.; Comerford, K.M.; Ginouves, A.; Fitzgerald, K.T.; Seeballuck, F.; Godson, C.; Nielsen, J.E.; Moynagh, P.; Pouyssegur, J.; Taylor, C.T.
Prolyl hydroxylase-1 negatively regulates IkappaB kinase-beta, giving insight into hypoxia-induced NFkappaB activity
Proc. Natl. Acad. Sci. USA
103
18154-18159
2006
Homo sapiens
Manually annotated by BRENDA team
Lobry, C.; Lopez, T.; Israel, A.; Weil, R.
Negative feedback loop in T cell activation through IkappaB kinase-induced phosphorylation and degradation of Bcl10
Proc. Natl. Acad. Sci. USA
104
908-913
2007
Homo sapiens
Manually annotated by BRENDA team
Olivotto, E.; Borzi, R.M.; Vitellozzi, R.; Pagani, S.; Facchini, A.; Battistelli, M.; Penzo, M.; Li, X.; Flamigni, F.; Li, J.; Falcieri, E.; Facchini, A.; Marcu, K.B.
Differential requirements for IKKalpha and IKKbeta in the differentiation of primary human osteoarthritic chondrocytes
Arthritis Rheum.
58
227-239
2008
Homo sapiens (O14920), Homo sapiens (O15111), Homo sapiens
Manually annotated by BRENDA team
Shaul, J.D.; Farina, A.; Huxford, T.
The human IKKbeta subunit kinase domain displays CK2-like phosphorylation specificity
Biochem. Biophys. Res. Commun.
374
592-597
2008
Homo sapiens (O14920), Homo sapiens
Manually annotated by BRENDA team
Lo, Y.C.; Maddineni, U.; Chung, J.Y.; Rich, R.L.; Myszka, D.G.; Wu, H.
High-affinity interaction between IKKbeta and NEMO
Biochemistry
47
3109-3116
2008
Homo sapiens (O14920)
Manually annotated by BRENDA team
Pandey, M.K.; Sung, B.; Kunnumakkara, A.B.; Sethi, G.; Chaturvedi, M.M.; Aggarwal, B.B.
Berberine modifies cysteine 179 of IkappaBalpha kinase, suppresses nuclear factor-kappaB-regulated antiapoptotic gene products, and potentiates apoptosis
Cancer Res.
68
5370-5379
2008
Homo sapiens (O14920)
Manually annotated by BRENDA team
Wilson, W.; Baldwin, A.S.
Maintenance of constitutive IkappaB kinase activity by glycogen synthase kinase-3alpha/beta in pancreatic cancer
Cancer Res.
68
8156-8163
2008
Homo sapiens (O14920), Homo sapiens (O15111)
Manually annotated by BRENDA team
Moreno-Maldonado, R.; Ramirez, A.; Navarro, M.; Fernandez-Acenero, M.J.; Villanueva, C.; Page, A.; Jorcano, J.L.; Bravo, A.; Llanos Casanova, M.
IKKalpha enhances human keratinocyte differentiation and determines the histological variant of epidermal squamous cell carcinomas
Cell Cycle
7
2021-2029
2008
Homo sapiens (O15111), Homo sapiens, Mus musculus (Q60680), Mus musculus
Manually annotated by BRENDA team
Dan, H.C.; Cooper, M.J.; Cogswell, P.C.; Duncan, J.A.; Ting, J.P.; Baldwin, A.S.
Akt-dependent regulation of NF-[kappa]B is controlled by mTOR and Raptor in association with IKK
Genes Dev.
22
1490-1500
2008
Homo sapiens (O14920), Homo sapiens (O15111)
Manually annotated by BRENDA team
Solt, L.A.; May, M.J.
The IkappaB kinase complex: master regulator of NF-kappaB signaling
Immunol. Res.
23
362-370
2008
Homo sapiens (O14920)
Manually annotated by BRENDA team
Mukherjee, S.; Negi, V.S.; Keitany, G.; Tanaka, Y.; Orth, K.
In vitro activation of the IkappaB kinase complex by human T-cell leukemia virus type-1 Tax
J. Biol. Chem.
283
15127-15133
2008
Homo sapiens
Manually annotated by BRENDA team
Cahill, C.M.; Rogers, J.T.
Interleukin (IL) 1beta induction of IL-6 is mediated by a novel phosphatidylinositol 3-kinase-dependent AKT/IkappaB kinase alpha pathway targeting activator protein-1
J. Biol. Chem.
283
25900-25912
2008
Homo sapiens (O15111)
Manually annotated by BRENDA team
Dan, H.C.; Baldwin, A.S.
Differential involvement of IkappaB kinases alpha and beta in cytokine- and insulin-induced mammalian target of rapamycin activation determined by Akt
J. Immunol.
180
7582-7589
2008
Mus musculus, Homo sapiens (O15111)
Manually annotated by BRENDA team
Lorenzo, P.; Alvarez, R.; Ortiz, M.A.; Alvarez, S.; Piedrafita, F.J.; de Lera, A.R.
Inhibition of IkappaB kinase-beta and anticancer activities of novel chalcone adamantyl arotinoids
J. Med. Chem.
51
5431-5440
2008
Homo sapiens (O14920)
Manually annotated by BRENDA team
Yan, S.S.; Li, Y.; Wang, Y.; Shen, S.S.; Gu, Y.; Wang, H.B.; Qin, G.W.; Yu, Q.
17-Acetoxyjolkinolide B irreversibly inhibits IkappaB kinase and induces apoptosis of tumor cells
Mol. Cancer Ther.
7
1523-1532
2008
Homo sapiens (O14920)
Manually annotated by BRENDA team
Ryu, M.J.; Anikin, V.; Hong, S.H.; Jeon, H.; Yu, Y.G.; Yu, M.H.; Chernysh, S.; Lee, C.
Activation of NF-kappaB by alloferon through down-regulation of antioxidant proteins and IkappaBalpha
Mol. Cell. Biochem.
313
91-102
2008
Homo sapiens (O15111), Homo sapiens
Manually annotated by BRENDA team
Chen, R.; Alvero, A.B.; Silasi, D.A.; Kelly, M.G.; Fest, S.; Visintin, I.; Leiser, A.; Schwartz, P.E.; Rutherford, T.; Mor, G.
Regulation of IKKbeta by miR-199a affects NF-kappaB activity in ovarian cancer cells
Oncogene
27
4712-4723
2008
Homo sapiens (O14920), Homo sapiens (O15111), Homo sapiens
Manually annotated by BRENDA team
Chen, R.A.; Ryzhakov, G.; Cooray, S.; Randow, F.; Smith, G.L.
Inhibition of IkappaB kinase by vaccinia virus virulence factor B14
PLoS Pathog.
4
e22
2008
Homo sapiens
Manually annotated by BRENDA team
Ha, K.H.; Byun, M.S.; Choi, J.; Jeong, J.; Lee, K.J.; Jue, D.M.
N-tosyl-L-phenylalanine chloromethyl ketone inhibits NF-kappaB activation by blocking specific cysteine residues of IkappaB kinase beta and p65/RelA
Biochemistry
48
7271-7278
2009
Homo sapiens
Manually annotated by BRENDA team
Kempson, J.; Guo, J.; Das, J.; Moquin, R.V.; Spergel, S.H.; Watterson, S.H.; Langevine, C.M.; Dyckman, A.J.; Pattoli, M.; Burke, J.R.; Yang, X.; Gillooly, K.M.; McIntyre, K.W.; Chen, L.; Dodd, J.H.; McKinnon, M.; Barrish, J.C.; Pitts, W.J.
Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IkappaB kinase
Bioorg. Med. Chem. Lett.
19
2646-2649
2009
Homo sapiens (O14920), Homo sapiens (Q15111)
Manually annotated by BRENDA team
Wu, J.P.; Fleck, R.; Brickwood, J.; Capolino, A.; Catron, K.; Chen, Z.; Cywin, C.; Emeigh, J.; Foerst, M.; Ginn, J.; Hrapchak, M.; Hickey, E.; Hao, M.H.; Kashem, M.; Li, J.; Liu, W.; Morwick, T.; Nelson, R.; Marshall, D.; Martin, L.; Nemoto, P.; Potocki, I.; Liuzzi, M.; Peet, G.W.; Scouten, E.; Stefany, D.; Turner, M.; Weldon, S.; Zimmitti, C.; Spero, D.; Kelly, T.A.
The discovery of thienopyridine analogues as potent IkappaB kinase beta inhibitors. Part II
Bioorg. Med. Chem. Lett.
19
5547-5551
2009
Homo sapiens
Manually annotated by BRENDA team
Sors, A.; Jean-Louis, F.; Begue, E.; Parmentier, L.; Dubertret, L.; Dreano, M.; Courtois, G.; Bachelez, H.; Michel, L.
Inhibition of IkappaB kinase subunit 2 in cutaneous T-cell lymphoma down-regulates nuclear factor-kappaB constitutive activation, induces cell death, and potentiates the apoptotic response to antineoplastic chemotherapeutic agents
Clin. Cancer Res.
14
901-911
2008
Homo sapiens
Manually annotated by BRENDA team
Tang, H.; Park, S.; Sun, S.C.; Trumbly, R.; Ren, G.; Tsung, E.; Yeung, K.C.
RKIP inhibits NF-kappaB in cancer cells by regulating upstream signaling components of the IkappaB kinase complex
FEBS Lett.
584
662-668
2010
Homo sapiens
Manually annotated by BRENDA team
Asamitsu, K.; Yamaguchi, T.; Nakata, K.; Hibi, Y.; Victoriano, A.F.; Imai, K.; Onozaki, K.; Kitade, Y.; Okamoto, T.
Inhibition of human immunodeficiency virus type 1 replication by blocking IkappaB kinase with noraristeromycin
J. Biochem.
144
581-589
2008
Homo sapiens
Manually annotated by BRENDA team
Clark, K.; Plater, L.; Peggie, M.; Cohen, P.
Use of the pharmacological inhibitor BX795 to study the regulation and physiological roles of TBK1 and IkappaB kinase epsilon: a distinct upstream kinase mediates Ser-172 phosphorylation and activation
J. Biol. Chem.
284
14136-14146
2009
Homo sapiens (Q14164)
Manually annotated by BRENDA team
Gan, Q.; Li, T.; Hu, B.; Lian, M.; Zheng, X.
HSCARG inhibits activation of NF-kappaB by interacting with IkappaB kinase-beta
J. Cell Sci.
122
4081-4088
2009
Homo sapiens
Manually annotated by BRENDA team
Kempson, J.; Spergel, S.H.; Guo, J.; Quesnelle, C.; Gill, P.; Belanger, D.; Dyckman, A.J.; Li, T.; Watterson, S.H.; Langevine, C.M.; Das, J.; Moquin, R.V.; Furch, J.A.; Marinier, A.; Dodier, M.; Martel, A.; Nirschl, D.; Van Kirk, K.; Burke, J.R.; Pattoli, M.A.; Gillooly, K.; McIntyre, K.W.; Chen, L.; Yang, Z.
Novel tricyclic inhibitors of IkappaB kinase
J. Med. Chem.
52
1994-2005
2009
Homo sapiens
Manually annotated by BRENDA team
Christopher, J.A.; Bamborough, P.; Alder, C.; Campbell, A.; Cutler, G.J.; Down, K.; Hamadi, A.M.; Jolly, A.M.; Kerns, J.K.; Lucas, F.S.; Mellor, G.W.; Miller, D.D.; Morse, M.A.; Pancholi, K.D.; Rumsey, W.; Solanke, Y.E.; Williamson, R.
Discovery of 6-aryl-7-alkoxyisoquinoline inhibitors of IkappaB kinase-beta (IKK-beta)
J. Med. Chem.
52
3098-3102
2009
Homo sapiens
Manually annotated by BRENDA team
Ochiai, T.; Saito, Y.; Saitoh, T.; Dewan, M.Z.; Shioya, A.; Kobayashi, M.; Kawachi, H.; Muto, S.; Itai, A.; Uota, S.; Eishi, Y.; Yamamoto, N.; Tanaka, S.; Arii, S.; Yamaoka, S.
Inhibition of IkappaB kinase beta restrains oncogenic proliferation of pancreatic cancer cells
J. Med. Dent. Sci.
55
49-59
2008
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Mbalaviele, G.; Sommers, C.D.; Bonar, S.L.; Mathialagan, S.; Schindler, J.F.; Guzova, J.A.; Shaffer, A.F.; Melton, M.A.; Christine, L.J.; Tripp, C.S.; Chiang, P.C.; Thompson, D.C.; Hu, Y.; Kishore, N.
A novel, highly selective, tight binding IkappaB kinase-2 (IKK-2) inhibitor: a tool to correlate IKK-2 activity to the fate and functions of the components of the nuclear factor-kappaB pathway in arthritis-relevant cells and animal models
J. Pharmacol. Exp. Ther.
329
14-25
2009
Rattus norvegicus, Homo sapiens (O14920), Homo sapiens (Q15111)
Manually annotated by BRENDA team
Gillooly, K.M.; Pattoli, M.A.; Taylor, T.L.; Chen, L.; Cheng, L.; Gregor, K.R.; Whitney, G.S.; Susulic, V.; Watterson, S.H.; Kempson, J.; Pitts, W.J.; Booth-Lute, H.; Yang, G.; Davies, P.; Kukral, D.W.; Strnad, J.; McIntyre, K.W.; Darienzo, C.J.; Salter-Cid, L.; Yang, Z.; Wang-Iverson, D.B.; Burke, J.R.
Periodic, partial inhibition of IkappaB kinase beta-mediated signaling yields therapeutic benefit in preclinical models of rheumatoid arthritis
J. Pharmacol. Exp. Ther.
331
349-360
2009
Canis lupus familiaris, Homo sapiens, Mus musculus, Rattus norvegicus
Manually annotated by BRENDA team
Mancino, A.; Habbeddine, M.; Johnson, E.; Luron, L.; Bebien, M.; Memet, S.; Fong, C.; Bajenoff, M.; Wu, X.; Karin, M.; Caamano, J.; Chi, H.; Seed, M.; Lawrence, T.
I kappa B kinase alpha (IKKalpha) activity is required for functional maturation of dendritic cells and acquired immunity to infection
EMBO J.
32
816-828
2013
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Gupta, S.C.; Prasad, S.; Reuter, S.; Kannappan, R.; Yadav, V.R.; Ravindran, J.; Hema, P.S.; Chaturvedi, M.M.; Nair, M.; Aggarwal, B.B.
Modification of cysteine 179 of IkappaBalpha kinase by nimbolide leads to down-regulation of NF-kappaB-regulated cell survival and proliferative proteins and sensitization of tumor cells to chemotherapeutic agents
J. Biol. Chem.
285
35406-35417
2010
Homo sapiens
Manually annotated by BRENDA team
Huang, W.; Hung, M.
Beyond NF-kappaB activation: Nuclear functions of IkappaB kinase alpha
J. Biomed. Sci.
20
3
2013
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Accardi, R.; Scalise, M.; Gheit, T.; Hussain, I.; Yue, J.; Carreira, C.; Collino, A.; Indiveri, C.; Gissmann, L.; Sylla, B.S.; Tommasino, M.
IkappaB kinase beta promotes cell survival by antagonizing p53 functions through DELTANp73alpha phosphorylation and stabilization
Mol. Cell. Biol.
31
2210-2226
2011
Homo sapiens
Manually annotated by BRENDA team
Mathialagan, S.; Poda, G.I.; Kurumbail, R.G.; Selness, S.R.; Hall, T.; Reitz, B.A.; Weinberg, R.A.; Kishore, N.; Mbalaviele, G.
Expression, purification and functional characterization of IkappaB kinase-2 (IKK-2) mutants
Protein Expr. Purif.
72
254-261
2010
Homo sapiens (O14920)
Manually annotated by BRENDA team
Masatani, T.; Ozawa, M.; Yamada, K.; Ito, N.; Horie, M.; Matsuu, A.; Okuya, K.; Tsukiyama-Kohara, K.; Sugiyama, M.; Nishizono, A.
Contribution of the interaction between the rabies virus P protein and I-kappa B kinase epsilon to the inhibition of type I IFN induction signalling
J. Gen. Virol.
97
316-326
2016
Homo sapiens
Manually annotated by BRENDA team
Deng, L.; Li, Y.; Ai, P.; Xie, Y.; Zhu, H.; Chen, N.
Increase in IkappaB kinase alpha expression suppresses the tumor progression and improves the prognosis for nasopharyngeal carcinoma
Mol. Carcinog.
54
156-165
2015
Homo sapiens
Manually annotated by BRENDA team
Xie, Y.; Li, Y.; Peng, X.; Peng, X.; Henderson, F.; Deng, L.; Chen, N.
Ikappa B kinase alpha involvement in the development of nasopharyngeal carcinoma through a NF-kappaB-independent and ERK-dependent pathway
Oral Oncol.
49
1113-1120
2013
Homo sapiens
Manually annotated by BRENDA team
Gao, S.; Wu, J.; Liang, L.; Xu, R.
RNF8 negatively regulates NF-kappaB signaling by targeting IkappaB kinase implications for the regulation of inflammation signaling
Biochem. Biophys. Res. Commun.
488
189-195
2017
Homo sapiens
Manually annotated by BRENDA team
Siddiqui, M.A.; Badruddeen, M.A.; Akhtar, J.; Uddin M S, S.; Irfan Khan, M.; Khalid, M.
Molecular mechanism of interactions between chrysin and I-kappa-B kinase epsilon (IKKe)/tank binding kinase-1(TBK1) Cell-based assay and in silico molecular docking studies
J. Biomol. Struct. Dyn.
38
589-596
2020
Homo sapiens (Q14164)
Manually annotated by BRENDA team
Anthony, N.G.; Baiget, J.; Berretta, G.; Boyd, M.; Breen, D.; Edwards, J.; Gamble, C.; Gray, A.I.; Harvey, A.L.; Hatziieremia, S.; Ho, K.H.; Huggan, J.K.; Lang, S.; Llona-Minguez, S.; Luo, J.L.; McIntosh, K.; Paul, A.; Plevin, R.J.; Robertson, M.N.; Scott, R.; Suckling, C.J.; Sutcliffe, O.B.; Young, L.C.; Mackey, S.P.
Inhibitory kappa B kinase alpha (IKKalpha) inhibitors that recapitulate their selectivity in cells against isoform-related biomarkers
J. Med. Chem.
60
7043-7066
2017
Homo sapiens (O14920), Homo sapiens (O15111)
Manually annotated by BRENDA team
Al-Shaer, M.A.; Almazari, I.S.; Taha, M.O.
Discovery of novel potent nuclear factor kappa-B inhibitors (IKK-beta) via extensive ligand-based modeling and virtual screening
J. Mol. Recognit.
30
e2604
2017
Homo sapiens (O14920)
Manually annotated by BRENDA team
Zheng, J.; Park, M.H.; Lee, H.P.; Hyun, B.K.; Chun, H.O.; Jung, S.H.; Seo, H.O.; Ham, Y.W.; Han, S.B.; Hong, J.T.
A small molecule, (E)-2-methoxy-4-(3-(4-methoxyphenyl) prop-1-en-1-yl) phenol suppresses tumor growth via inhibition of IkappaB kinase beta in colorectal cancer in vivo and in vitro
Oncotarget
8
91258-91269
2017
Homo sapiens (O14920)
Manually annotated by BRENDA team