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

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


The taxonomic range for the selected organisms is: Homo sapiens

EC NUMBER
COMMENTARY hide
2.7.11.10
-
RECOMMENDED NAME
GeneOntology No.
IkappaB kinase
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
ATP + [IkappaB protein] = ADP + [IkappaB phosphoprotein]
show the reaction diagram
activation and reaction mechanism
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phospho group transfer
SYSTEMATIC NAME
IUBMB Comments
ATP:[IkappaB protein] phosphotransferase
The enzyme phosphorylates IkappaB proteins at specific serine residues, which marks them for destruction via the ubiquitination pathway. Subsequent degradation of the IkB complex (IKK) activates NF-kappaB, a translation factor that plays an important role in inflammation, immunity, cell proliferation and apoptosis. If the serine residues are replaced by threonine residues, the activity of the enzyme is decreased considerably.
CAS REGISTRY NUMBER
COMMENTARY hide
159606-08-3
-
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
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
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
ATP + Bcl
ADP + phosphorylated Bcl
show the reaction diagram
ATP + Bcl
ADP + phosphorylated Bcl10
show the reaction diagram
-
Bcl10 is phosphorylated by the NEMO/IKK complex, recombinant substrate GST-Bcl10 expressed in HEK-293T cells, degradation of Bcl
-
-
?
ATP + Bcl10
ADP + phosphorylated Bcl10
show the reaction diagram
-
negative regulatory activity of the IKK complex in Bcl10 degradation, which is part of the regulatory mechanisms that precisely control the response to antigens, overview
-
-
?
ATP + GST-IkappaBalpha
ADP + GST-IkappaBalpha phosphoprotein
show the reaction diagram
-
activity assay
-
-
?
ATP + IkappaB alpha
ADP + phosphorylated IkappaB alpha
show the reaction diagram
-
-
-
-
?
ATP + IkappaB protein
ADP + IkappaB phosphoprotein
show the reaction diagram
-
-
-
-
?
ATP + IkappaBalpha
ADP + phosphorylated IkappaBalpha
show the reaction diagram
ATP + interferon regulatory factor 3
ADP + phosphorylated interferon regulatory factor 3
show the reaction diagram
-
-
-
-
?
ATP + KKKKERLLDDRHDSGLDSMKDEE
ADP + phosphorylated-KKKKERLLDDRHDSGLDSMKDEE
show the reaction diagram
-
IKK substrate peptide derived from IkappaBalpha sequence
-
-
?
ATP + NF-kappaB p65 subunit
ADP + phosphorylated NF-kappaB p65 subunit
show the reaction diagram
-
IKKalpha and IKKbeta phosphorylate NF-kappaB p65 subunit at Ser536
-
-
?
ATP + p65/RelA
ADP + phosphorylated p65/RelA
show the reaction diagram
-
-
-
-
?
ATP + STAT1 transcription factor
ADP + phosphorylated STAT1 transcription factor
show the reaction diagram
-
-
-
-
?
ATP + [acetylated histone H3 protein]
ADP + [acetylated histone H3 phosphoprotein]
show the reaction diagram
ATP + [biotinylated IkappaBa peptide]
ADP + [biotinylated IkappaBa phosphopeptide]
show the reaction diagram
-
i.e. biotin-Gly-Leu-Lys-Lys-Glu-Arg-Leu-Leu-Asp-Asp-Arg-His-Asp-Ser32-Gly-Leu-Asp-Ser36-Met-Lys-Asp-Glu-Glu
-
-
?
ATP + [DELTANp73alpha protein]
ADP + [DELTANp73alpha phosphoprotein]
show the reaction diagram
-
phosphorylation at Ser422 by IKKbeta, IKKbeta is inactive with S422A mutant substrate. DELTANp73alpha i a dominant negative inhibitor of p53 and p73
-
-
?
ATP + [GST-IkappaB protein]
ADP + [GST-IkappaB phosphoprotein]
show the reaction diagram
-
-
-
-
?
ATP + [GST-IkappaBalpha protein]
ADP + [GST-IkappaBalpha phosphoprotein]
show the reaction diagram
-
-
-
-
?
ATP + [GST-IkappaBalpha1-54 protein]
ADP + [GST-IkappaBalpha1-54 phosphoprotein]
show the reaction diagram
-
-
-
-
?
ATP + [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 SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
ATP + Bcl
ADP + phosphorylated Bcl
show the reaction diagram
-
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 + [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+
-
-
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)phenyl)acetic acid
-
IC50 for the IKKbeta is 0.0022 mM
(E)-4-[3-(5-(adamant-1-yl)-2-(but-1-oxy)-4-(2-methoxyethoxymethoxy)-phenyl)-3-oxoprop-1-en-1-yl]benzoic acid
-
shows highest inhibition of IKKbeta and highest induction of apoptosis in Jurkat cells
(E)-4-[3-(5-(adamant-1-yl)-2-(hexyl-1-oxy)-4-(2-methoxyethoxymethoxy)phenyl)-3-oxoprop-1-en-1-yl]benzoic acid
-
exhibits improved anti-IKKbeta and growth inhibitory activities and has lost its RAR-dependent transactivation function
(E)-4-[3-(5-(adamant-1-yl)-2-ethoxy-4-(2-methoxyethoxymethoxy)phenyl)-3-oxoprop-1-en-1-yl]benzoic acid
-
-
(E)-4-[3-(5-(adamant-1-yl)-4-(2-methoxyethoxymethoxy)-2-(pentyl-1-oxy)phenyl)-3-oxoprop-1-en-1-yl]benzoic acid
-
-
(E)-4-[3-(5-(adamant-1-yl)-4-(2-methoxyethoxymethoxy)-2-(prop-2-en-1-oxy)phenyl)-3-oxoprop-1-en-1-yl]benzoic acid
-
-
(E)-4-[3-(5-(adamant-1-yl)-4-(2-methoxyethoxymethoxy)-2-(prop-2-yn-1-oxy)phenyl)-3-oxoprop-1-en-1-yl]benzoic acid
-
shows highest inhibition of IKKbeta and highest induction of apoptosis in Jurkat cells
(E)-4-[3-(5-(adamant-1-yl)-4-(2-methoxyethoxymethoxy)-2-phenylmethoxy-phenyl)-3-oxoprop-1-en-1-yl]benzoic acid
-
exhibits improved anti-IKKbeta and growth inhibitory activities and has lost its RAR-dependent transactivation function
(E)-4-[3-(5-adamant-1-yl-4-(2-methoxyethoxymethoxy)-2-(prop-1-oxy)-phenyl)-3-oxoprop-1-en-1-yl]benzoic acid
-
-
1-(4-chlorophenyl)-4-ureido-1H-pyrazole-3-carboxamide
-
i.e. SC-108
1-(6-chloro-9H-beta-carbolin-8-yl)-3-methylurea
-
inhibits IKK with IC50 of 0.02 mM
1-(benzo[d][1,3]dioxol-5-yl)-8-(3-chloroisonicotinamido)-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide
-
i.e. PHA-379
1-(benzo[d][1,3]dioxol-5-yl)-8-(5-chloro-2-(4-methylpiperazin-1-yl)isonicotinamido)-4,5-dihydro-1H-benzo-[g]indazole-3-carboxamide
-
i.e. PHA-250
1-[3-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanamine
-
-
1-[4-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanamine
-
-
1-[4-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanesulfonamide
-
-
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-fluorophenyl)-8-methyl-N-[2-(piperidin-1-yl)ethyl]-8H-imidazo[4,5-d][1,3]thiazolo[5,4-b]pyridin-5-amine
-
-
2-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzoic acid
-
IC50 for the IKK complex is above 0.1 mM
2-amino-6-(2-hydroxy-6-isobutoxyphenyl)-4-(piperidin-3-yl)nicotinonitrile
-
i.e. PHA-535E
2-benzamido-pyrimidines
-
diverse derivatives, synthesis and inhibitory potential determination, overview
2-hydroxy-N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]acetamide
-
-
2-methanesulfonyl-4-methyl-7-methylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
-
2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7yl)pyridin-2-yl)methyl)acetamide
-
BMS-066, inhibitor of IKKbeta
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-(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-(5-(3-acetamino-3-methylbutyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
-
IC50 for the IKK complex is 800 nM
4-(5-(3-amino-3-ethylpentyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
-
IC50 for the IKK complex is 30 nM
4-(5-(3-amino-3-methyl-but-1-ynyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
-
IC50 for the IKK complex is 200 nM
4-(5-(3-amino-3-methyl-butyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
-
IC50 for the IKK complex is 40 nM
4-(5-(3-hydroxy-3-methylbutyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amin
-
IC50 for the IKK complex is 50 nM, cellular profile
4-(5-(3-methoxypropyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
-
IC50 for the IKK complex is 100 nM, cellular profile
4-(5-(4-hydroxybutyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
-
IC50 for the IKK complex is 40 nM, cellular profile
4-(7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]isoquinolin-6-yl)benzenesulfonamide
-
-
4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzoic acid
-
IC50 for the IKK complex is 0.018 mM, cellular profile
4-methyl-7-methylamino-2-(azepan-1-yl)-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
-
4-methyl-7-methylamino-2-(methylthio)-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
-
4-methyl-7-methylamino-2-benzylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
-
4-methyl-7-methylamino-2-cyclopentylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
-
4-methyl-7-methylamino-2-diethylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
-
4-methyl-7-methylamino-2-ethylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
-
4-methyl-7-methylamino-2-hydroxyethylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
-
4-methyl-7-methylamino-2-methylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
-
4-methyl-7-methylamino-2-methylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
-
4-methyl-7-methylamino-2-piperidine-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
-
4-methyl-7-methylamino-2-thienylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
-
4-methyl-7-methylamino-2-[1,2,3,6-tetrahydropyridine]-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
-
-
4-[7-(benzyloxy)isoquinolin-6-yl]benzenesulfonamide
-
-
4-[7-(piperidin-3-ylmethoxy)isoquinolin-6-yl]benzenesulfonamide
-
-
4-[7-(piperidin-3-yloxy)isoquinolin-6-yl]benzenesulfonamide
-
-
4-[7-(piperidin-4-ylmethoxy)isoquinolin-6-yl]benzenesulfonamide
-
-
4-[7-(piperidin-4-yloxy)isoquinolin-6-yl]benzenesulfonamide
-
-
4-[7-[(1-acetylpiperidin-4-yl)oxy]isoquinolin-6-yl]benzenesulfonamide
-
-
5,6-dibromo-beta-carboline
-
inhibits IKK with IC50 of 600 nM
5-((3-fluorophenyl)ethynyl)-2-ureidothiophene-3-carboxamide
-
i.e. PHA-966
5-(4-fluorophenyl)-2-ureidothiophene-3-carboxamide
-
i.e. SC-440
5-amino-2,30-bithiophene-4-carboxamide
-
i.e. SC-514
5-Aminosalicylate
-
weak inhibition of IKK-2
5-bromo-6-chloro-beta-carboline
-
inhibits IKK with IC50 of 600 nM
5-bromo-6-cyano-beta-carboline
-
inhibits IKK with IC50 of 0.0011 mM
5-bromo-6-fluoro-beta-carboline
-
inhibits IKK with IC50 of 0.002 mM
5-bromo-6-methoxy-beta-carboline
-
nonspecific inhibitor of IKK, inhibits IKK with IC50 of 0.004 mM
5-bromo-6-trifluoromethyl-beta-carboline
-
inhibits IKK with IC50 of 0.0011 mM
5-bromo-beta-carboline
-
inhibits IKK with IC50 of 0.015 mM
6,8-dichloro-7-(cyclohexylmethoxy)-9H-beta-carboline
-
inhibits IKK with IC50 of 0.003 mM
6,8-dichloro-7-ethoxy-9H-beta-carboline
-
inhibits IKK with IC50 of 140 nM
6,8-dichloro-7-methoxy-9H-beta-carboline
-
inhibits IKK with IC50 of 170 nM
6,8-dichloro-9H-beta-carbolin-7-yl morpholine-4-carboxylate
-
inhibits IKK with IC50 of 0.0032 mM
6,8-dichloro-beta-carboline
-
inhibits IKK with IC50 of 200 nM
-
6-bromo-7-(piperidin-4-yloxy)isoquinoline
-
-
6-bromo-7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]isoquinoline
-
-
6-phenyl-7-(piperidin-3-ylmethoxy)isoquinoline
-
-
6-phenyl-7-(piperidin-3-yloxy)isoquinoline
-
-
6-phenyl-7-(piperidin-4-ylmethoxy)isoquinoline
-
-
6-phenyl-7-(piperidin-4-yloxy)isoquinoline
-
-
6-phenyl-7-(pyridin-3-ylmethoxy)isoquinoline
-
-
6-phenyl-7-(pyridin-4-ylmethoxy)isoquinoline
-
-
7-(2-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
-
-
7-(3-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
-
-
7-(3-methoxyphenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
-
-
7-(4-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
-
;
7-(OCH2CH(CH2CH2))-6,8-dichloro-beta-carboline
-
inhibits IKK with IC50 of 80 nM
-
7-(piperidin-4-yloxy)isoquinoline
-
-
7-hydroxy-6,8-dichloro-beta-carboline
-
inhibits IKK with IC50 of 0.011 mM
-
7-[(1-acetylpiperidin-4-yl)oxy]-6-bromoisoquinoline
-
-
7-[(1-acetylpiperidin-4-yl)oxy]-6-phenylisoquinoline
-
-
7-[3-(aminomethyl)phenyl]-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
-
-
7-[[1-(ethylsulfonyl)piperidin-4-yl]methoxy]-6-phenylisoquinoline
-
-
7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]-6-phenylisoquinoline
-
-
8-(5-chloro-2-(4-methylpiperazin-1-yl)isonicotinamido)-1-(4-fluorophenyl)-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide
-
PHA-408, ATP-competitive, selective IKK-2 inhibitor; 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
BX795
-
-
-
chalcone
-
-
COMPOUND A
-
leads to a significant reduction of Panc-1 cell and MiaPaCa-2 cell growth
curcumin
-
weak inhibition of IKK-2
cyclopentenone prostaglandins
cyclopentenone prostanoids
-
inhibition of IKK and thus inhibition of NFkappaB-mediated HSV-1-induced HIV-1 replication
cyclopentone prostaglandines
-
inhibition of IKK-2
ethanol,N-[2-[[2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-yl]amino]ethyl]
-
-
evodiamine
-
alkaloid extracted from Evodia rutaecarpa fruits exhibiting antiproliferative, antimetastatic, and apoptotic activities, inhibits IKKalpha activity, suppresses IKKalpha phosphorylation and degradation, and specifically blocks NF-kappaB activation by IKK and other agents, translocation, and activity, overview
IMD-0354
-
specific IKKbeta inhibition
LY294002
-
phosphorylation of IKKalphaT23 is inhibited both by LY294002 and wortmannin, but phosphorylation of Ser176/Ser180 is not
methyl (6-chloro-9H-beta-carbolin-8-yl)carbamate
-
inhibits IKK with IC50 of 700 nM
methyl 1-(3-amino-2-carbamoyl-4-propylthieno[2,3-b]pyridin-6-yl)piperidine-4-carboxylate
-
-
MX781
-
0.02 mM inhibit IKKbeta by 65% in the presence of an ATP concentration corresponding to its Km value
N,1-dimethyl-7-phenyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
-
;
N,1-dimethyl-7-phenyl-1H-pyrazolo[5,1-b]purin-4-amine
-
-
N,3,8-trimethyl-2-phenyl-3,8-dihydrodiimidazo[4,5-b:4',5'-d]pyridin-5-amine
-
;
N,8-dimethyl-2-phenyl-8H-imidazo[4,5-d][1,3]oxazolo[5,4-b]pyridin-5-amine
-
;
N,8-dimethyl-2-phenyl-8H-imidazo[4,5-d][1,3]thiazolo[5,4-b]pyridin-5-amine
-
;
N,N-dimethyl-3-[(4-[[(6-phenylisoquinolin-7-yl)oxy]methyl]piperidin-1-yl)sulfonyl]propan-1-amine
-
-
N-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)ethane-1,2-diamine
-
-
N-(2-aminoethyl)-4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzamide
-
IC50 for the IKK complex is 0.0044 mM
N-(2-dimethyl-aminoethyl)-4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzamide
-
IC50 for the IKK complex is 300 nM, cellular profile
N-(2-pyrrolidin-1-yl-ethyl)-4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzamide
-
IC50 for the IKK complex is 500 nM
N-(3,5-bis-trifluoromethylphenyl)-5-chloro-2-hydroxybenzamide
-
-
N-(3-methyl-butyl)-4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzamide
-
IC50 for the IKKbeta is above 0.1 mM
N-(6-chloro-9H-beta-carbolin-8-yl)-2-(pyridin-2-yl)acetamide
-
inhibits IKK with IC50 of 0.003 mM
N-(6-chloro-9H-beta-carbolin-8-yl)-2-methoxybenzamide
-
inhibits IKK with IC50 of 0.02 mM
N-(6-chloro-9H-beta-carbolin-8-yl)-3-methoxybenzamide
-
inhibits IKK with IC50 of 600 nM
N-(6-chloro-9H-beta-carbolin-8-yl)-4-hydroxybutanamide
-
inhibits IKK with IC50 of 0.02 mM
N-(6-chloro-9H-beta-carbolin-8-yl)-4-methoxybenzamide
-
inhibits IKK with IC50 of 0.0013 mM
N-(6-chloro-9H-beta-carbolin-8-yl)acetamide
-
inhibits IKK with IC50 of 600 nM
N-(6-chloro-9H-beta-carbolin-8-yl)benzamide
-
inhibits IKK with IC50 of 700 nM
N-(6-chloro-9H-beta-carbolin-8-yl)benzenesulfonamide
-
inhibits IKK with IC50 of 0.02 mM
N-(6-chloro-9H-beta-carbolin-8-yl)methanesulfonamide
-
inhibits IKK with IC50 of 0.0083 mM
N-(6-chloro-9H-beta-carbolin-8-yl)morpholine-4-carboxamide
-
inhibits IKK with IC50 of 0.02 mM
N-(6-chloro-9H-beta-carbolin-8-yl)pyridine-2-carboxamide
-
inhibits IKK with IC50 of 0.001 mM
N-(6-chloro-9H-beta-carbolin-8-yl)pyridine-4-carboxamide
-
inhibits IKK with IC50 of 300 nM
N-(8-methyl-2-phenylimidazo[1,2-a]thieno[3,2-e]pyrazin-5-yl)ethane-1,2-diamine
-
-
N-acetylcysteine
-
inhibits phosphorylation of IkappaBalpha
N-benzyl-6-chloro-9H-beta-carbolin-8-amine
-
inhibits IKK with IC50 of 0.02 mM
N-ethyl-2-(4-fluorophenyl)-N-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine
-
-
N-methyl-2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine
-
-
N-tosyl-L-phenylalanine chloromethyl ketone
-
-
N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]-1,2,3-thiadiazole-4-carboxamide
-
;
N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]acetamide
-
;
N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]butanediamide
-
-
N-[5-[4-(cyclopropylamino)-1-methyl-1H-pyrazolo[5,1-b]purin-7-yl]-2-fluorobenzyl]acetamide
-
-
N-[[2-fluoro-5-[8-methyl-5-methylamino-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]acetamide
-
-
N-[[2-fluoro-5-[8-methyl-5-methylamino-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]methanesulfonamide
-
-
N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]-1,2,3-thiadiazole-5-amide
-
-
N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]acetamide
-
-
N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]isoxazole-5-amide
-
-
N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]methanesulfonamide
-
-
N1-(1,8-dimethylimidazo-[1,2-a]quinoxalin-4-yl)ethane-1,2-diamine
-
i.e. PHA-068E
N2,N2-dimethyl-N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]glycinamide
-
-
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; suppresses IKK activity potentailly through dissociation of raptor from the mTOR complex
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; 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; 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; 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
0.0022
(4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)phenyl)acetic acid
Homo sapiens;
-
IC50 for the IKKbeta is 0.0022 mM
0.00052 - 0.0043
1,4-dimethyl-7-methylamino-2-phenyl-4H-imidazo[4,5-d]imidazo[5,4-b]pyridine
0.02
1-(6-chloro-9H-beta-carbolin-8-yl)-3-methylurea
Homo sapiens;
-
inhibits IKK with IC50 of 0.02 mM
0.0008 - 0.0126
1-[3-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanamine
0.0001 - 0.0063
1-[4-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanamine
0.0004 - 0.004
1-[4-[7-(piperidin-4-yloxy)isoquinolin-6-yl]phenyl]methanesulfonamide
0.0003
17-acetoxyjolkinolide B
Homo sapiens;
-
-
0.000056 - 0.0083
2-(4-fluorophenyl)-8-methyl-N-[2-(piperidin-1-yl)ethyl]-8H-imidazo[4,5-d][1,3]thiazolo[5,4-b]pyridin-5-amine
0.1
2-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzoic acid
Homo sapiens;
-
IC50 for the IKK complex is above 0.1 mM
0.000025
2-hydroxy-N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]acetamide
Homo sapiens;
-
-
0.000081 - 0.0076
2-methanesulfonyl-4-methyl-7-methylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
0.000009 - 0.00496
2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7yl)pyridin-2-yl)methyl)acetamide
0.001
3-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzoic acid
Homo sapiens;
-
IC50 for the IKKbeta is 0.001 mM
0.0027
3-amino-4,6-dimethylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.0169
3-amino-4-(1-benzofuran-2-yl)-6-methylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.0108
3-amino-4-(2-methoxyethoxy)thieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.014
3-amino-4-(4-chlorophenyl)-6-methylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.02
3-amino-4-(4-hydroxyphenyl)-6-methylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta, larger than 0.0200
0.002
3-amino-4-ethoxythieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.0011
3-amino-4-furan-2-yl-6-methylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.0047
3-amino-4-methoxythieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.0025
3-amino-4-methyl-6-morpholin-4-ylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.00068
3-amino-4-methyl-6-piperazin-1-ylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.0024
3-amino-4-methyl-6-piperidin-1-ylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.0022
3-amino-4-propoxythieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.000072
3-amino-6-(1,4-diazepan-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.0029
3-amino-6-(2-aminoethoxy)-4-methylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.0066
3-amino-6-(2-hydroxyethoxy)-4-methylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.00063
3-amino-6-(3-aminoazepan-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.05
3-amino-6-(3-aminopropoxy)-4-methylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta, larger than 0.0500
0.0024
3-amino-6-(3-hydroxypiperidin-1-yl)-4-methylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.00057 - 0.0133
3-amino-6-(3-hydroxypiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
0.0051
3-amino-6-(3-hydroxypropoxy)-4-methylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.00014
3-amino-6-(3-oxo-1,4-diazepan-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.002
3-amino-6-(3-oxopiperazin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.000041 - 0.0016
3-amino-6-(4-aminopiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
0.00015
3-amino-6-(4-carbamoylpiperazin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.0013
3-amino-6-(4-carbamoylpiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.00075
3-amino-6-(4-hydroxypiperidin-1-yl)-4-methylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.00028 - 0.0112
3-amino-6-(4-hydroxypiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
0.00068
3-amino-6-(4-methoxypiperidin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.00052
3-amino-6-(4-methylpiperazin-1-yl)-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.0025
3-amino-6-methyl-4-(2-methylpropyl)thieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.0085
3-amino-6-methyl-4-(4-methylphenyl)thieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.0074
3-amino-6-methyl-4-phenylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.0013
3-amino-6-methyl-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.006
3-amino-6-methyl-4-pyridin-2-ylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.002
3-amino-6-methyl-4-thiophen-2-ylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.0013
3-amino-6-methyl-4-[4-(methylsulfonyl)phenyl]thieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.0127
3-amino-6-methylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.00012 - 0.0034
3-amino-6-piperazin-1-yl-4-propylthieno[2,3-b]pyridine-2-carboxamide
0.0058
3-amino-6-[(2-hydroxyethyl)amino]-4-methylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.0005
3-amino-6-[(3R)-3-aminopyrrolidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.00195
3-amino-6-[(3R)-3-hydroxypyrrolidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.00059
3-amino-6-[(3S)-3-aminopyrrolidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.00145
3-amino-6-[(3S)-3-hydroxypyrrolidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.00068
3-amino-6-[4-(dimethylamino)piperidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.00012
3-amino-6-[4-(methylamino)piperidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.000098
3-amino-6-[4-[(methylsulfonyl)amino]piperidin-1-yl]-4-propylthieno[2,3-b]pyridine-2-carboxamide
Homo sapiens;
-
IKKbeta
0.000012 - 0.00262
3-methoxy-N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]propanamide
0.000007
3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzonitrile
Homo sapiens;
-
-
0.0079 - 0.0251
3-[7-(benzyloxy)isoquinolin-6-yl]benzenesulfonamide
0.0013 - 0.0079
3-[7-(piperidin-4-yloxy)isoquinolin-6-yl]benzenesulfonamide
0.00025
4-(1-benzothiophen-2-yl)-N-[3-chloro-4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
Homo sapiens;
-
IC50 for the IKK complex is 250 nM
0.00015
4-(1-benzothiophen-2-yl)-N-[3-methoxy-4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
Homo sapiens;
-
IC50 for the IKK complex is 150 nM
0.0085
4-(1-benzothiophen-2-yl)-N-[4-(pyrrolidin-1-ylcarbonyl)phenyl]pyrimidin-2-amine
Homo sapiens;
-
IC50 for the IKK complex is 0.0085 mM, cellular profile
0.00008
4-(1-benzothiophen-2-yl)-N-[4-([4-(dimethyl-amino)piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
Homo sapiens;
-
IC50 for the IKK complex is 80 nM, cellular profile
0.00007
4-(1-benzothiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
Homo sapiens;
-
IC50 for the IKK complex is 70 nM, cellular profile
0.0008
4-(5-(3-acetamino-3-methylbutyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
Homo sapiens;
-
IC50 for the IKK complex is 800 nM
0.00003
4-(5-(3-amino-3-ethylpentyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
Homo sapiens;
-
IC50 for the IKK complex is 30 nM
0.0002
4-(5-(3-amino-3-methyl-but-1-ynyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
Homo sapiens;
-
IC50 for the IKK complex is 200 nM
0.00004
4-(5-(3-amino-3-methyl-butyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
Homo sapiens;
-
IC50 for the IKK complex is 40 nM
0.00005
4-(5-(3-hydroxy-3-methylbutyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amin
Homo sapiens;
-
IC50 for the IKK complex is 50 nM, cellular profile
0.0001
4-(5-(3-methoxypropyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
Homo sapiens;
-
IC50 for the IKK complex is 100 nM, cellular profile
0.00004
4-(5-(4-hydroxybutyl)thiophen-2-yl)-N-[4-([4-pyrrolidin-1-yl-piperidin-1-yl]carbonyl)phenyl]pyrimidin-2-amine
Homo sapiens;
-
IC50 for the IKK complex is 40 nM, cellular profile
0.001 - 0.0251
4-(7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]isoquinolin-6-yl)benzenesulfonamide
0.018
4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzoic acid
Homo sapiens;
-
IC50 for the IKK complex is 0.018 mM, cellular profile
0.00013
4-methyl-7-methylamino-2-(azepan-1-yl)-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
Homo sapiens;
-
IKK-2
0.000028 - 0.0026
4-methyl-7-methylamino-2-(methylthio)-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
0.0015
4-methyl-7-methylamino-2-benzylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
Homo sapiens;
-
IKK-2
0.00016
4-methyl-7-methylamino-2-cyclopentylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
Homo sapiens;
-
IKK-2
0.0025 - 0.02
4-methyl-7-methylamino-2-diethylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
0.000015 - 0.0011
4-methyl-7-methylamino-2-ethylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
0.0003
4-methyl-7-methylamino-2-hydroxyethylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
Homo sapiens;
-
IKK-2
0.000015 - 0.00084
4-methyl-7-methylamino-2-methylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
0.00092 - 0.0034
4-methyl-7-methylamino-2-methylamino-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
0.000011 - 0.00027
4-methyl-7-methylamino-2-phenyl-4H-imidazo[4,5-d]oxazolo[5,4-b]pyridine
0.000006 - 0.0035
4-methyl-7-methylamino-2-phenyl-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
0.00021 - 0.0061
4-methyl-7-methylamino-2-piperidine-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
0.000015
4-methyl-7-methylamino-2-thienylamido-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
Homo sapiens;
-
IKK-2
0.000033 - 0.0081
4-methyl-7-methylamino-2-[1,2,3,6-tetrahydropyridine]-4H-imidazo[4,5-d]thiazolo[5,4-b]pyridine
0.0032 - 0.0251
4-[7-(benzyloxy)isoquinolin-6-yl]benzenesulfonamide
0.0008 - 0.005
4-[7-(piperidin-3-ylmethoxy)isoquinolin-6-yl]benzenesulfonamide
0.0008 - 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
0.0006
5,6-dibromo-beta-carboline
Homo sapiens;
-
inhibits IKK with IC50 of 600 nM
0.0006
5-bromo-6-chloro-beta-carboline
Homo sapiens;
-
inhibits IKK with IC50 of 600 nM
0.0011
5-bromo-6-cyano-beta-carboline
Homo sapiens;
-
inhibits IKK with IC50 of 0.0011 mM
0.002
5-bromo-6-fluoro-beta-carboline
Homo sapiens;
-
inhibits IKK with IC50 of 0.002 mM
0.004
5-bromo-6-methoxy-beta-carboline
Homo sapiens;
-
nonspecific inhibitor of IKK, inhibits IKK with IC50 of 0.004 mM
0.0011
5-bromo-6-trifluoromethyl-beta-carboline
Homo sapiens;
-
inhibits IKK with IC50 of 0.0011 mM
0.015
5-bromo-beta-carboline
Homo sapiens;
-
inhibits IKK with IC50 of 0.015 mM
0.003
6,8-dichloro-7-(cyclohexylmethoxy)-9H-beta-carboline
Homo sapiens;
-
inhibits IKK with IC50 of 0.003 mM
0.00014
6,8-dichloro-7-ethoxy-9H-beta-carboline
Homo sapiens;
-
inhibits IKK with IC50 of 140 nM
0.00017
6,8-dichloro-7-methoxy-9H-beta-carboline
Homo sapiens;
-
inhibits IKK with IC50 of 170 nM
0.0032
6,8-dichloro-9H-beta-carbolin-7-yl morpholine-4-carboxylate
Homo sapiens;
-
inhibits IKK with IC50 of 0.0032 mM
0.0002
6,8-dichloro-beta-carboline
Homo sapiens;
-
inhibits IKK with IC50 of 200 nM
-
0.0004 - 0.01
6-bromo-7-(piperidin-4-yloxy)isoquinoline
0.005 - 0.0251
6-bromo-7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]isoquinoline
0.0002 - 0.0032
6-phenyl-7-(piperidin-3-ylmethoxy)isoquinoline
0.0006 - 0.004
6-phenyl-7-(piperidin-3-yloxy)isoquinoline
0.0013 - 0.01
6-phenyl-7-(piperidin-4-ylmethoxy)isoquinoline
0.0001 - 0.0025
6-phenyl-7-(piperidin-4-yloxy)isoquinoline
0.004 - 0.0251
6-phenyl-7-(pyridin-3-ylmethoxy)isoquinoline
0.005 - 0.0251
6-phenyl-7-(pyridin-4-ylmethoxy)isoquinoline
0.000044
7-(2-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
Homo sapiens;
-
-
0.000007
7-(3-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
Homo sapiens;
-
-
0.000008
7-(3-methoxyphenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
Homo sapiens;
-
-
0.000043 - 0.00173
7-(4-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
0.00008
7-(OCH2CH(CH2CH2))-6,8-dichloro-beta-carboline
Homo sapiens;
-
inhibits IKK with IC50 of 80 nM
-
0.005 - 0.0251
7-(piperidin-4-yloxy)isoquinoline
0.011
7-hydroxy-6,8-dichloro-beta-carboline
Homo sapiens;
-
inhibits IKK with IC50 of 0.011 mM
-
0.0126 - 0.0251
7-[(1-acetylpiperidin-4-yl)oxy]-6-bromoisoquinoline
0.0016 - 0.0032
7-[(1-acetylpiperidin-4-yl)oxy]-6-phenylisoquinoline
0.000011
7-[3-(aminomethyl)phenyl]-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
Homo sapiens;
-
-
0.0025 - 0.02
7-[[1-(ethylsulfonyl)piperidin-4-yl]methoxy]-6-phenylisoquinoline
0.002 - 0.0126
7-[[1-(ethylsulfonyl)piperidin-4-yl]oxy]-6-phenylisoquinoline
0.00004 - 0.0141
8-(5-chloro-2-(4-methylpiperazin-1-yl)isonicotinamido)-1-(4-fluorophenyl)-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide
0.0013
8-amino-6-chloro-beta-carboline
Homo sapiens;
-
inhibits IKK with IC50 of 0.0013 mM
0.0018
8-dimethylamino-6-chloro-beta-carboline
Homo sapiens;
-
inhibits IKK with IC50 of 0.0018 mM
0.00018 - 0.02
8-methyl-2-(4-fluorophenyl)-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine
0.0018
8-methylamino-6-chloro-beta-carboline
Homo sapiens;
-
inhibits IKK with IC50 of 0.0018 mM
0.004
8-nitro-6-chloro-beta-carboline
Homo sapiens;
-
inhibits IKK with IC50 of 0.004 mM
0.000033 - 0.005
acetamide,N-[2-[[2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-yl]amino]ethyl]
0.000041
BX795
Homo sapiens;
-
-
-
0.007
chalcone
Homo sapiens;
-
-
0.000075 - 0.0086
ethanol,N-[2-[[2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-yl]amino]ethyl]
0.0007
methyl (6-chloro-9H-beta-carbolin-8-yl)carbamate
Homo sapiens;
-
inhibits IKK with IC50 of 700 nM
0.0078
methyl 1-(3-amino-2-carbamoyl-4-propylthieno[2,3-b]pyridin-6-yl)piperidine-4-carboxylate
Homo sapiens;
-
IKKbeta
0.00004 - 0.00167
N,1-dimethyl-7-phenyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
0.000034 - 0.00099
N,1-dimethyl-7-phenyl-1H-pyrazolo[5,1-b]purin-4-amine
0.00052 - 0.00428
N,3,8-trimethyl-2-phenyl-3,8-dihydrodiimidazo[4,5-b:4',5'-d]pyridin-5-amine
0.000011 - 0.00027
N,8-dimethyl-2-phenyl-8H-imidazo[4,5-d][1,3]oxazolo[5,4-b]pyridin-5-amine
0.000006 - 0.0035
N,8-dimethyl-2-phenyl-8H-imidazo[4,5-d][1,3]thiazolo[5,4-b]pyridin-5-amine
0.0013 - 0.01
N,N-dimethyl-3-[(4-[[(6-phenylisoquinolin-7-yl)oxy]methyl]piperidin-1-yl)sulfonyl]propan-1-amine
0.0003 - 0.004
N-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)ethane-1,2-diamine
0.0044
N-(2-aminoethyl)-4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzamide
Homo sapiens;
-
IC50 for the IKK complex is 0.0044 mM
0.0003
N-(2-dimethyl-aminoethyl)-4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzamide
Homo sapiens;
-
IC50 300 nM for the IK cellular profile
0.0005
N-(2-pyrrolidin-1-yl-ethyl)-4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzamide
Homo sapiens;
-
IC50 for the IKK complex is 500 nM
0.1
N-(3-methyl-butyl)-4-([4-(1-benzothiophen-2-yl)pyrimidin-2-yl]amino)benzamide
Homo sapiens;
-
IC50 for the IKKbeta is above 0.1 mM
0.003
N-(6-chloro-9H-beta-carbolin-8-yl)-2-(pyridin-2-yl)acetamide
Homo sapiens;
-
inhibits IKK with IC50 of 0.003 mM
0.02
N-(6-chloro-9H-beta-carbolin-8-yl)-2-methoxybenzamide
Homo sapiens;
-
inhibits IKK with IC50 of 0.02 mM
0.0006
N-(6-chloro-9H-beta-carbolin-8-yl)-3-methoxybenzamide
Homo sapiens;
-
inhibits IKK with IC50 of 600 nM
0.02
N-(6-chloro-9H-beta-carbolin-8-yl)-4-hydroxybutanamide
Homo sapiens;
-
inhibits IKK with IC50 of 0.02 mM
0.0013
N-(6-chloro-9H-beta-carbolin-8-yl)-4-methoxybenzamide
Homo sapiens;
-
inhibits IKK with IC50 of 0.0013 mM
0.0006
N-(6-chloro-9H-beta-carbolin-8-yl)acetamide
Homo sapiens;
-
inhibits IKK with IC50 of 600 nM
0.0007
N-(6-chloro-9H-beta-carbolin-8-yl)benzamide
Homo sapiens;
-
inhibits IKK with IC50 of 700 nM
0.02
N-(6-chloro-9H-beta-carbolin-8-yl)benzenesulfonamide
Homo sapiens;
-
inhibits IKK with IC50 of 0.02 mM
0.0083
N-(6-chloro-9H-beta-carbolin-8-yl)methanesulfonamide
Homo sapiens;
-
inhibits IKK with IC50 of 0.0083 mM
0.02
N-(6-chloro-9H-beta-carbolin-8-yl)morpholine-4-carboxamide
Homo sapiens;
-
inhibits IKK with IC50 of 0.02 mM
0.001
N-(6-chloro-9H-beta-carbolin-8-yl)pyridine-2-carboxamide
Homo sapiens;
-
inhibits IKK with IC50 of 0.001 mM
0.0003
N-(6-chloro-9H-beta-carbolin-8-yl)pyridine-4-carboxamide
Homo sapiens;
-
inhibits IKK with IC50 of 300 nM
0.000019 - 0.0004
N-(8-methyl-2-phenylimidazo[1,2-a]thieno[3,2-e]pyrazin-5-yl)ethane-1,2-diamine
0.02
N-benzyl-6-chloro-9H-beta-carbolin-8-amine
Homo sapiens;
-
inhibits IKK with IC50 of 0.02 mM
0.000039 - 0.0034
N-ethyl-2-(4-fluorophenyl)-N-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine
0.000026 - 0.0031
N-methyl-2-(4-fluorophenyl)-8-methyl-8H-imidazo[4,5-d]thiazolo[5,4-b]pyridine-5-amine
0.000039 - 0.00015
N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]-1,2,3-thiadiazole-4-carboxamide
0.000014 - 0.000633
N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]acetamide
0.000022
N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]butanediamide
Homo sapiens;
-
-
0.00028 - 0.0097
N-[5-[4-(cyclopropylamino)-1-methyl-1H-pyrazolo[5,1-b]purin-7-yl]-2-fluorobenzyl]acetamide
0.000053 - 0.0035
N-[[2-fluoro-5-[8-methyl-5-methylamino-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]acetamide
0.000032 - 0.0042
N-[[2-fluoro-5-[8-methyl-5-methylamino-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]methanesulfonamide
0.000016 - 0.001
N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]-1,2,3-thiadiazole-5-amide
0.000022 - 0.0019
N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]acetamide
0.000025 - 0.0014
N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]isoxazole-5-amide
0.000005 - 0.001
N-[[3-[8-methyl-5-(methylamino)-8H-imidazo[4,5-d]-thiazolo[5,4-b]pyridine-2-yl]phenyl]methyl]methanesulfonamide
0.000079
N2,N2-dimethyl-N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]glycinamide
Homo sapiens;
-
-
0.00037 - 0.00064
noraristeromycin
0.0001
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
37
-
assay at
additional information
-
assay caried out at room temperature
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
; microRNA hsa-miR-199a regulates IKKbeta expression in epithelial ovarian cancer cells (EOC)
Manually annotated by BRENDA team
-
chronically infected with HIV-1
Manually annotated by BRENDA team
-
bronchial epithelial cell line
Manually annotated by BRENDA team
-
cell line KG-1
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
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epidermal
Manually annotated by BRENDA team
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respiratory tract mucosa
Manually annotated by BRENDA team
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Namalva cell line
Manually annotated by BRENDA team
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primary
Manually annotated by BRENDA team
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mycosis fungoides cell line
Manually annotated by BRENDA team
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lung adenocarcinoma cell line
Manually annotated by BRENDA team
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; microRNA hsa-miR-199a regulates IKKbeta expression in epithelial ovarian cancer cells (EOC)
Manually annotated by BRENDA team
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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
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in T-cells
Manually annotated by BRENDA team
additional information
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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
PDB
SCOP
CATH
UNIPROT
ORGANISM
Homo sapiens;
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
700000
-
IKK complex
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
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
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
cytoplasmic extracts are prepared
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native IkappaBalpha kinase from HeLa S3 cells by ammonium sulfate fractionation, ultrafiltration, and gel filtration
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nuclear and cytoplasmic extracts are prepared
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recombinant C-terminally FLAG-tagged wild-type and mutant IKK-2s
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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
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recombinant His-tagged IKKbeta from Sf21 insect cells by nickel affinity chromatography
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using Ni-NTA-chromatography
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Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
a Flag-tagged IKKbeta expression vector is used
-
a GST-IkappaBalpha fusion protein is generated; a GST-IkappaBalpha fusion protein is generated
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coexpression of FLAG-atgged wild-type and mutant IKKbeta proteins with T7-tagged IKKgamma and HA-tagged ubiquitin in 293T cells
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coexpression of FLAG-tagged IKKbeta, T7-tagged IKKgamma, and Tax in 293T cells and in murine embryonic fibroblasts devoid of the enzyme
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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
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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
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expressed in baculovirus-infected Sf9 cells
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expressed in baculovirus-infected sf9 insect cells
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expressed in Escherichia coli as a His-tagged fusion protein
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expression of C-terminally FLAG-tagged wild-type and mutant IKK-2s
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expression of FLAG- or HA-tagged wild-type and mutant IKKbeta in HEK-293 and HeLa cells
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expression of GST-tagged IKKalpha and IKKbeta in HEK-293 cells, coexpression of IKKbeta and GFP-tagged DELTANp73alpha protein in HEK-293 cells
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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
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expression of Myc-tagged IKK-alpha or IKK-beta in mouse embryonic fibroblasts MEF cell line
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expression of wild-type FLAG-tagged IKK-beta or FLAG-tagged IKK-beta mutant C179A in A-293 cells
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Flag-IKKalpha and Flag-IKKbeta vectors for transfection of HEK293 cells are used
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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
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into the vector pSC-b for sequencing, subsequently into pCMV-FLAG-1 or pEBG6P
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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
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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
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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
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transient expression of wild-type and mutant FLAG-tagged IKK2 in HELF cells
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transient expression of wild-type and mutant IKKbeta in HeLa cells
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EXPRESSION
ORGANISM
UNIPROT
LITERATURE
IKKalpha and IKKbeta downregulation in 38E6E7HFK cells by siRNA expression
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the enzyme is underexpressed in highly invasive SUNE-1-5-8F cells compared with non-invasive cells (SUNE-1 and SUNE-6-10B)
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ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
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
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deletion mutant containing residues 640-756, which contains the entire C-terminal region after the HLH domain, interacts well with NEMO
DELTA1-680
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deletion mutant wich stably interacts with NEMO
DELTA1-705
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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
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deletion mutant containing only the 11-residues of the NEMO-binding region (NBD) is not sufficient for interaction with NEMO
DELTA307-384
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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
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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
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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
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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
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site-directed mutagenesis, the mutant has lost the time-dependent binding of inhibitor PHA-408
F26W
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site-directed mutagenesis
K106N
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site-directed mutagenesis
K106Q
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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
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site-directed mutagenesis, ubiquitination and phosphorylation of the mutant is unaltered compared to the wild-type IKKbeta
K147R
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site-directed mutagenesis, reduced monoubiquitination of IKKbeta mutant
K163R
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site-directed mutagenesis, monoubiquitination-defective mutant of IKKbeta retaining kinase activity in Tax-expressing cells
K171R
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site-directed mutagenesis, ubiquitination and phosphorylation of the mutant is unaltered compared to the wild-type IKKbeta
K18R
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site-directed mutagenesis, ubiquitination and phosphorylation of the mutant is unaltered compared to the wild-type IKKbeta
K198R
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site-directed mutagenesis, ubiquitination and phosphorylation of the mutant is unaltered compared to the wild-type IKKbeta
K234R
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site-directed mutagenesis, ubiquitination and phosphorylation of the mutant is unaltered compared to the wild-type IKKbeta
K238R
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site-directed mutagenesis, monoubiquitination-defective mutant of IKKbeta
K254R
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site-directed mutagenesis, ubiquitination and phosphorylation of the mutant is unaltered compared to the wild-type IKKbeta
K275R
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site-directed mutagenesis, ubiquitination and phosphorylation of the mutant is unaltered compared to the wild-type IKKbeta
K44A
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site-directed mutagenesis of subunit IKK2, catalytically inactive mutant and no NF-kappaB stimulation in infected cells in vivo
K44R
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site-directed mutagenesis, monoubiquitination-defective mutant of IKKbeta
L353X
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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
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IKKalpha mutant, defective in HLH domains, unable to bind wild-type Vav-1
M96L
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site-directed mutagenesis
P191A
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inactive IKKbeta mutant
S176E/S180E
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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
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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
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site-directed mutagenesis, the mutant shows time-dependent inhibition by PHA-408 like the wild-type
additional information
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
drug development
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because of its central role in the overall NF-kappaB regulation, IKK-2 is a viable target for drug discovery
medicine
molecular biology
pharmacology