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Literature summary for 2.7.11.10 extracted from

  • 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 (2009), J. Pharmacol. Exp. Ther., 329, 14-25.
    View publication on PubMed
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Application

Application Comment Organism
medicine PHA-408 is efficacious in a chronic model of arthritis with no adverse effects Rattus norvegicus
medicine PHA-408 is efficacious in a chronic model of arthritis with no adverse effects Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
-
 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
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 Homo sapiens
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 Rattus norvegicus

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens O14920
-
-
Homo sapiens Q15111
-
-
Rattus norvegicus
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
blood
-
 Homo sapiens
-
liver
-
 Rattus norvegicus
-
paw
-
 Rattus norvegicus
-
peripheral blood mononuclear cell
-
 Homo sapiens
-
rheumatoid arthritis disease specific synovial fibroblast
-
 Homo sapiens
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
IkappaB kinase-1
-
 Homo sapiens
IkappaB kinase-2
-
 Rattus norvegicus
IkappaB kinase-2
-
 Homo sapiens
IKK-1
-
 Homo sapiens
IKK-2
-
 Rattus norvegicus
IKK-2
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
 activity assay Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.6
-
 activity assay Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Rattus norvegicus
ATP
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000006
-
 8-(5-chloro-2-(4-methylpiperazin-1-yl)isonicotinamido)-1-(4-fluorophenyl)-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00004
-
-
 Homo sapiens 8-(5-chloro-2-(4-methylpiperazin-1-yl)isonicotinamido)-1-(4-fluorophenyl)-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide
0.0141
-
-
 Homo sapiens 8-(5-chloro-2-(4-methylpiperazin-1-yl)isonicotinamido)-1-(4-fluorophenyl)-4,5-dihydro-1H-benzo[g]indazole-3-carboxamide