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Literature summary extracted from

  • Gillooly, K.M.; Pattoli, M.A.; Taylor, T.L.; Chen, L.; Cheng, L.; Gregor, K.R.; Whitney, G.S.; Susulic, V.; Watterson, S.H.; Kempson, J.; Pitts, W.J.; Booth-Lute, H.; Yang, G.; Davies, P.; Kukral, D.W.; Strnad, J.; McIntyre, K.W.; Darienzo, C.J.; Salter-Cid, L.; Yang, Z.; Wang-Iverson, D.B.; Burke, J.R.
    Periodic, partial inhibition of IkappaB kinase beta-mediated signaling yields therapeutic benefit in preclinical models of rheumatoid arthritis (2009), J. Pharmacol. Exp. Ther., 331, 349-360.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.11.10
-
 Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.10 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 Canis lupus familiaris
2.7.11.10 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 Homo sapiens
2.7.11.10 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 Mus musculus
2.7.11.10 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 Rattus norvegicus
2.7.11.10 4-(2'-aminoethyl)amino-1,8-dimethylimidazo(1,2-a)quinoxaline BMS-345541, inhibitor of IKKbeta Canis lupus familiaris
2.7.11.10 4-(2'-aminoethyl)amino-1,8-dimethylimidazo(1,2-a)quinoxaline BMS-345541, inhibitor of IKKbeta Homo sapiens
2.7.11.10 4-(2'-aminoethyl)amino-1,8-dimethylimidazo(1,2-a)quinoxaline BMS-345541, inhibitor of IKKbeta Mus musculus
2.7.11.10 4-(2'-aminoethyl)amino-1,8-dimethylimidazo(1,2-a)quinoxaline BMS-345541, inhibitor of IKKbeta Rattus norvegicus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.11.10 ATP + [IkappaB protein] Mus musculus
-
 ADP + [IkappaB phosphoprotein]
-
 ?
2.7.11.10 ATP + [IkappaB protein] Homo sapiens
-
 ADP + [IkappaB phosphoprotein]
-
 ?
2.7.11.10 ATP + [IkappaB protein] Rattus norvegicus
-
 ADP + [IkappaB phosphoprotein]
-
 ?
2.7.11.10 ATP + [IkappaB protein] Canis lupus familiaris
-
 ADP + [IkappaB phosphoprotein]
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.10 Canis lupus familiaris
-
-
-
2.7.11.10 Homo sapiens
-
-
-
2.7.11.10 Mus musculus
-
-
-
2.7.11.10 Rattus norvegicus
-
 Lewis rat
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.7.11.10
-
 Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.11.10 blood
-
 Mus musculus
-
2.7.11.10 blood
-
 Homo sapiens
-
2.7.11.10 blood
-
 Rattus norvegicus
-
2.7.11.10 blood
-
 Canis lupus familiaris
-
2.7.11.10 peripheral blood mononuclear cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.10 ATP + [IkappaB protein]
-
 Mus musculus ADP + [IkappaB phosphoprotein]
-
 ?
2.7.11.10 ATP + [IkappaB protein]
-
 Homo sapiens ADP + [IkappaB phosphoprotein]
-
 ?
2.7.11.10 ATP + [IkappaB protein]
-
 Rattus norvegicus ADP + [IkappaB phosphoprotein]
-
 ?
2.7.11.10 ATP + [IkappaB protein]
-
 Canis lupus familiaris ADP + [IkappaB phosphoprotein]
-
 ?

Subunits

EC Number Subunits Comment Organism
2.7.11.10 oligomer the multisubunit IkappaB kinase complex is composed of two catalytic subunits, IKKalpha and IKKbeta, and a regulatory subunit termed NEMO or IKKgamma Mus musculus
2.7.11.10 oligomer the multisubunit IkappaB kinase complex is composed of two catalytic subunits, IKKalpha and IKKbeta, and a regulatory subunit termed NEMO or IKKgamma Homo sapiens
2.7.11.10 oligomer the multisubunit IkappaB kinase complex is composed of two catalytic subunits, IKKalpha and IKKbeta, and a regulatory subunit termed NEMO or IKKgamma Rattus norvegicus
2.7.11.10 oligomer the multisubunit IkappaB kinase complex is composed of two catalytic subunits, IKKalpha and IKKbeta, and a regulatory subunit termed NEMO or IKKgamma Canis lupus familiaris

Synonyms

EC Number Synonyms Comment Organism
2.7.11.10 IkappaB kinase
-
 Mus musculus
2.7.11.10 IkappaB kinase
-
 Homo sapiens
2.7.11.10 IkappaB kinase
-
 Rattus norvegicus
2.7.11.10 IkappaB kinase
-
 Canis lupus familiaris
2.7.11.10 IKK
-
 Mus musculus
2.7.11.10 IKK
-
 Homo sapiens
2.7.11.10 IKK
-
 Rattus norvegicus
2.7.11.10 IKK
-
 Canis lupus familiaris

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.7.11.10 30
-
 activity assay Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.7.11.10 7.2
-
 activity assay Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.10 ATP
-
 Mus musculus
2.7.11.10 ATP
-
 Homo sapiens
2.7.11.10 ATP
-
 Rattus norvegicus
2.7.11.10 ATP
-
 Canis lupus familiaris

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.11.10 0.000009
-
 IKKbeta catalyzed phosphorylation of IkappaBalpha Homo sapiens 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7yl)pyridin-2-yl)methyl)acetamide
2.7.11.10 0.00029
-
 IkappaBalpha phosphorylation in peripheral blood mononuclear cell Homo sapiens 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7yl)pyridin-2-yl)methyl)acetamide
2.7.11.10 0.00496
-
 IKKalpha catalyzed phosphorylation of IkappaBalpha Homo sapiens 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

General Information

EC Number General Information Comment Organism
2.7.11.10 physiological function the IkappaB kinase complex is essential in transducing the signal-inducible activation of the transcription factor NF-kappaB in response to proinflammatory stimuli Mus musculus
2.7.11.10 physiological function the IkappaB kinase complex is essential in transducing the signal-inducible activation of the transcription factor NF-kappaB in response to proinflammatory stimuli Homo sapiens
2.7.11.10 physiological function the IkappaB kinase complex is essential in transducing the signal-inducible activation of the transcription factor NF-kappaB in response to proinflammatory stimuli Rattus norvegicus
2.7.11.10 physiological function the IkappaB kinase complex is essential in transducing the signal-inducible activation of the transcription factor NF-kappaB in response to proinflammatory stimuli Canis lupus familiaris