Any feedback?
Please rate this page
(enzyme.php)
(0/150)

BRENDA support

BRENDA Home
show all | hide all No of entries

Information on EC 2.7.11.10 - IkappaB kinase

for references in articles please use BRENDA:EC2.7.11.10
Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
EC Tree
     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.
Specify your search results
Select one or more organisms in this record: ?
This record set is specific for:
UNIPROT: O14920
Show additional data
Do not include text mining results
Include (text mining) results
Include results (AMENDA + additional results, but less precise)
Word Map
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
IkappaB alpha kinase
-
IkappaB kinase beta
-
IkappaB kinase-2
-
inhibitor kappa-B kinase-beta
-
inhibitor of nuclear factor kappa B kinase beta subunit inhibitor of nuclear factor kappa-B kinase alpha subunit
-
inhibitory kappa B kinase beta
-
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
-
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
the I kappa B/NF-kappa B system is a key determinant of mucosal inflammation and protection
-
-
?
ATP + IkappaBalpha
ADP + phosphorylated IkappaBalpha
show the reaction diagram
ATP + p65/RelA
ADP + phosphorylated p65/RelA
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 + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
show the reaction diagram
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 + a protein
ADP + a phosphoprotein
show the reaction diagram
the I kappa B/NF-kappa B system is a key determinant of mucosal inflammation and protection
-
-
?
ATP + [IkappaB protein]
ADP + [IkappaB phosphoprotein]
show the reaction diagram
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(1R,4R)-4-(2-amino-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-cyclohexanol
-
(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-(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-[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
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-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-hydroxy-N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]acetamide
-
2-[[bis(2-hydroxyethyl)amino]methyl]-4-(2-methylbutan-2-yl)phenol
NCI0079692, 59% inhibition at 0.1 mM
3-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimdin-4-yl)benzamide
-
3-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-benzenesulfonamide
-
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
-
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-(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-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-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-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-amine
-
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-[N'-(4,6-dimethylpyrimidin-2-yl)carbamimidamido]-N-(phenylcarbamoyl)benzene-1-sulfonamide
NCI0107328, 94% inhibition at 0.1 mM
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
6,6-dimethyl-1-[3-[3-(3-nitrophenoxy)propoxy]phenyl]-1,3,5-triazinane-2,4-diimine
NCI0111727, 75% inhibition at 0.1 mM
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-[3-(aminomethyl)phenyl]-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
-
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
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
COMPOUND A
leads to a significant reduction of Panc-1 cell and MiaPaCa-2 cell growth
lysyl-N-(4-methoxynaphthalen-2-yl)alaninamide
NCI0339925, 93% inhibition at 0.1 mM
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,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-(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-[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
-
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
-
PHA-408
a selective IKK-2 inhibitor, shows time-dependent binding to the enzyme
Rapamycin
suppresses IKK activity potentailly through dissociation of raptor from the mTOR complex
additional information
structure-based design of IKK-2 inhibitors based on induced-fit docking into the homology model, overview
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
glycogen synthase kinase-3beta
GSK-3 is required for constitutive IKK activity
-
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
-
raptor
raptor (mTOR associated protein) controls phosphorylation of IkappaBalpha and p65/RelA as shown by knockdown of raptor in PC3 cells
-
TNF-alpha
-
-
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
0.03
(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
0.03
(R)-2-amino-4-(2-(hydroximethyl)pyrrolidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.03
(R)-2-amino-4-(3-hydroxypyrrolidin-1-yl)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.03
(S)-2-amino-4-(2-(hydroximethyl)pyrrolidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.0059
1-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-sulfonamide
Homo sapiens
at pH 7.5 and 30°C
0.0003
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
0.0036
2-amino-4-((1R,2S,3R,4S)-2,3,4-trihydroxycyclopentylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.03
2-amino-4-((1R,4R)-4-hydroxycyclohexylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.03
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
0.03
2-amino-4-((1RS,2SR,3RS)-2,3-dihydroxycyclopentylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.03
2-amino-4-((cyclopropylmethyl)amino)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.03
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
0.03
2-amino-4-(2-fluorophenyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.03
2-amino-4-(2-hydroxyethylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.03
2-amino-4-(2-hydroxyphenyl)-77H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.03
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
2-amino-4-(3-(hydroxymethyl)phenyl)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.03
2-amino-4-(3-fluorophenyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.03
2-amino-4-(3-hydroxypropylamino)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.0038
2-amino-4-(3-hydroyphenyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
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
2-amino-4-(4-(methylsulfonyl)phenyl)-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.03
2-amino-4-(4-fluorophenyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.0023
2-amino-4-(4-hydroxymethyl)phenyl-7H-pyrrolo[2,3-d]-pyrimidine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
0.02
2-amino-4-(4-hydroxyphenyl)-7H-pyrrolo[2,3-d]pyrimdine-5-carbonitrile
Homo sapiens
at pH 7.5 and 30°C
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
0.03
2-amino-4-(benzylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.03
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
0.03
2-amino-4-(cyclohexylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.03
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
0.03
2-amino-4-(methylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.03
2-amino-4-(phenylamino)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.03
2-amino-4-(piperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.03
2-amino-4-chloro-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.02
2-amino-4-morpholino-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.03
2-amino-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
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
-
0.03
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
0.0059
3-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-benzenesulfonamide
Homo sapiens
at pH 7.5 and 30°C
0.000012
3-methoxy-N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]propanamide
Homo sapiens
-
0.000007
3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzonitrile
Homo sapiens
-
0.03
4-((2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-benzenesulfonamide
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.03
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
0.03
4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimdin-4-yl)benzamide
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.001
4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-benzenesulfonamide
Homo sapiens
at pH 7.5 and 30°C
0.0014
4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-N-(p-tolyl)-benzenesulfonamide
Homo sapiens
at pH 7.5 and 30°C
0.0001
4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-N-methylbenzenesulfonamide
Homo sapiens
at pH 7.5 and 30°C
0.00061
4-(2-amino-7H-pyrrol[2,3-d]pyrimidin-4-yl)benzenesulfonamide
Homo sapiens
at pH 7.5 and 30°C
0.03
4-(5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)benzenesulfonamide
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.0025
4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)benzenesulfonamide
Homo sapiens
at pH 7.5 and 30°C
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
0.03
4-chloro-7H-pyrrolo[2,3-d]pyrimidin-2-amine
Homo sapiens
IC50 above 0.03 mM, at pH 7.5 and 30°C
0.000011
4-[N'-(4,6-dimethylpyrimidin-2-yl)carbamimidamido]-N-(phenylcarbamoyl)benzene-1-sulfonamide
Homo sapiens
at 37°C, pH not specified in the publication
0.000044
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
7-(4-fluorophenyl)-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
Homo sapiens
-
0.000011
7-[3-(aminomethyl)phenyl]-N,1-dimethyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
Homo sapiens
-
0.00004
8-(5-chloro-2-(4-methylpiperazin-1-yl)isonicotinamido)-1-(4-fluorophenyl)-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide
Homo sapiens
-
0.007
chalcone
Homo sapiens
-
0.01681
lysyl-N-(4-methoxynaphthalen-2-yl)alaninamide
Homo sapiens
at 37°C, pH not specified in the publication
0.00004
N,1-dimethyl-7-phenyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine
Homo sapiens
-
0.00052
N,3,8-trimethyl-2-phenyl-3,8-dihydrodiimidazo[4,5-b:4',5'-d]pyridin-5-amine
Homo sapiens
-
0.000011
N,8-dimethyl-2-phenyl-8H-imidazo[4,5-d][1,3]oxazolo[5,4-b]pyridin-5-amine
Homo sapiens
-
0.000006
N,8-dimethyl-2-phenyl-8H-imidazo[4,5-d][1,3]thiazolo[5,4-b]pyridin-5-amine
Homo sapiens
-
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
N-(4-(2-amino-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)-methanesulfonamide
Homo sapiens
at pH 7.5 and 30°C
0.000039
N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]-1,2,3-thiadiazole-4-carboxamide
Homo sapiens
-
0.000014
N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]acetamide
Homo sapiens
-
0.000022
N-[3-[1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl]benzyl]butanediamide
Homo sapiens
-
0.000079
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
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.4
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
37
assay at
additional information
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
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
microRNA hsa-miR-199a regulates IKKbeta expression in epithelial ovarian cancer cells (EOC)
Manually annotated by BRENDA team
additional information
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
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?
IKKB_HUMAN
756
0
86564
Swiss-Prot
other Location (Reliability: 2)
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
dimer
gel filtration
oligomer
two catalytic subunits, IKK1 and IKK2
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phosphoprotein
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
C179A
berberine does not have any effect on mutant IKK beta C179A. This proves that berberine inhibits IKK beta activity through the modification of Cys179
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
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
M96L
site-directed mutagenesis
S177E/S181E
ectopic overexpression of a constitutively active form of IKKbeta in Type II epithelial ovarian cancer cells (EOC) results in a significant decrease in IkappaBalpha expression
Y169F
site-directed mutagenesis, the mutant shows time-dependent inhibition by PHA-408 like the wild-type
additional information
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
recombinant C-terminally FLAG-tagged wild-type and mutant IKK-2s
using Ni-NTA-chromatography
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
a GST-IkappaBalpha fusion protein is generated
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
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
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
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
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
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
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
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
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
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
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