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Literature summary for 2.7.11.10 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
Search for more literature for 2.7.11.10

Cloned(Commentary)

Cloned (Comment) Organism
-
 Homo sapiens

Inhibitors

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

Natural Substrates/ Products (Substrates)

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

Organism

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

Purification (Commentary)

Purification (Comment) Organism
-
 Homo sapiens

Source Tissue

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

Substrates and Products (Substrate)

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

Subunits

Subunits Comment Organism
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
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
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
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

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

Temperature Optimum [°C]

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

pH Optimum

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

Cofactor

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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
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
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

General Information Comment Organism
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
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
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
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