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Literature summary for 2.7.11.10 extracted from

  • Castro, A.C.; Dang, L.C.; Soucy, F.; Grenier, L.; Mazdiyasni, H.; Hottelet, M.; Parent, L.; Pien, C.; Palombella, V.; Adams, J.
    Novel IKK inhibitors: beta-carbolines (2003), Bioorg. Med. Chem. Lett., 13, 2419-2422.
    View publication on PubMed
Search for more literature for 2.7.11.10

Activating Compound

Activating Compound Comment Organism Structure
additional information IKK is induced by TNFalpha Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-(6-chloro-9H-beta-carbolin-8-yl)-3-methylurea inhibits IKK with IC50 of 0.02 mM Homo sapiens
5,6-dibromo-beta-carboline inhibits IKK with IC50 of 600 nM Homo sapiens
5-bromo-6-chloro-beta-carboline inhibits IKK with IC50 of 600 nM Homo sapiens
5-bromo-6-cyano-beta-carboline inhibits IKK with IC50 of 0.0011 mM Homo sapiens
5-bromo-6-fluoro-beta-carboline inhibits IKK with IC50 of 0.002 mM Homo sapiens
5-bromo-6-methoxy-beta-carboline nonspecific inhibitor of IKK, inhibits IKK with IC50 of 0.004 mM Homo sapiens
5-bromo-6-trifluoromethyl-beta-carboline inhibits IKK with IC50 of 0.0011 mM Homo sapiens
5-bromo-beta-carboline inhibits IKK with IC50 of 0.015 mM Homo sapiens
6,8-dichloro-7-(cyclohexylmethoxy)-9H-beta-carboline inhibits IKK with IC50 of 0.003 mM Homo sapiens
6,8-dichloro-7-ethoxy-9H-beta-carboline inhibits IKK with IC50 of 140 nM Homo sapiens
6,8-dichloro-7-methoxy-9H-beta-carboline inhibits IKK with IC50 of 170 nM Homo sapiens
6,8-dichloro-9H-beta-carbolin-7-yl morpholine-4-carboxylate inhibits IKK with IC50 of 0.0032 mM Homo sapiens
6,8-dichloro-beta-carboline inhibits IKK with IC50 of 200 nM Homo sapiens
7-(OCH2CH(CH2CH2))-6,8-dichloro-beta-carboline inhibits IKK with IC50 of 80 nM Homo sapiens
7-hydroxy-6,8-dichloro-beta-carboline inhibits IKK with IC50 of 0.011 mM Homo sapiens
8-amino-6-chloro-beta-carboline inhibits IKK with IC50 of 0.0013 mM Homo sapiens
8-dimethylamino-6-chloro-beta-carboline inhibits IKK with IC50 of 0.0018 mM Homo sapiens
8-methylamino-6-chloro-beta-carboline inhibits IKK with IC50 of 0.0018 mM Homo sapiens
8-nitro-6-chloro-beta-carboline inhibits IKK with IC50 of 0.004 mM Homo sapiens
methyl (6-chloro-9H-beta-carbolin-8-yl)carbamate inhibits IKK with IC50 of 700 nM Homo sapiens
N-(6-chloro-9H-beta-carbolin-8-yl)-2-(pyridin-2-yl)acetamide inhibits IKK with IC50 of 0.003 mM Homo sapiens
N-(6-chloro-9H-beta-carbolin-8-yl)-2-methoxybenzamide inhibits IKK with IC50 of 0.02 mM Homo sapiens
N-(6-chloro-9H-beta-carbolin-8-yl)-3-methoxybenzamide inhibits IKK with IC50 of 600 nM Homo sapiens
N-(6-chloro-9H-beta-carbolin-8-yl)-4-hydroxybutanamide inhibits IKK with IC50 of 0.02 mM Homo sapiens
N-(6-chloro-9H-beta-carbolin-8-yl)-4-methoxybenzamide inhibits IKK with IC50 of 0.0013 mM Homo sapiens
N-(6-chloro-9H-beta-carbolin-8-yl)acetamide inhibits IKK with IC50 of 600 nM Homo sapiens
N-(6-chloro-9H-beta-carbolin-8-yl)benzamide inhibits IKK with IC50 of 700 nM Homo sapiens
N-(6-chloro-9H-beta-carbolin-8-yl)benzenesulfonamide inhibits IKK with IC50 of 0.02 mM Homo sapiens
N-(6-chloro-9H-beta-carbolin-8-yl)methanesulfonamide inhibits IKK with IC50 of 0.0083 mM Homo sapiens
N-(6-chloro-9H-beta-carbolin-8-yl)morpholine-4-carboxamide inhibits IKK with IC50 of 0.02 mM Homo sapiens
N-(6-chloro-9H-beta-carbolin-8-yl)pyridine-2-carboxamide inhibits IKK with IC50 of 0.001 mM Homo sapiens
N-(6-chloro-9H-beta-carbolin-8-yl)pyridine-4-carboxamide inhibits IKK with IC50 of 300 nM Homo sapiens
N-benzyl-6-chloro-9H-beta-carbolin-8-amine inhibits IKK with IC50 of 0.02 mM Homo sapiens
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 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + [IkappaBalpha protein] Homo sapiens enzyme is involved in activation of pro-inflammation signalling ADP + [IkappaBalpha phosphoprotein]
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
 isozymes IKK1 and IKK2
-

Source Tissue

Source Tissue Comment Organism Textmining
HeLa cell induced by TNFalpha Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + [GST-IkappaBalpha protein]
-
 Homo sapiens ADP + [GST-IkappaBalpha phosphoprotein]
-
 ?
ATP + [IkappaBalpha protein] enzyme is involved in activation of pro-inflammation signalling Homo sapiens ADP + [IkappaBalpha phosphoprotein]
-
 ?

Synonyms

Synonyms Comment Organism
IKK
-
 Homo sapiens
IKK complex
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00008
-
 inhibits IKK with IC50 of 80 nM Homo sapiens 7-(OCH2CH(CH2CH2))-6,8-dichloro-beta-carboline
0.0001
-
 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 Homo sapiens PS-1145
0.00014
-
 inhibits IKK with IC50 of 140 nM Homo sapiens 6,8-dichloro-7-ethoxy-9H-beta-carboline
0.00017
-
 inhibits IKK with IC50 of 170 nM Homo sapiens 6,8-dichloro-7-methoxy-9H-beta-carboline
0.0002
-
 inhibits IKK with IC50 of 200 nM Homo sapiens 6,8-dichloro-beta-carboline
0.0003
-
 inhibits IKK with IC50 of 300 nM Homo sapiens N-(6-chloro-9H-beta-carbolin-8-yl)pyridine-4-carboxamide
0.0006
-
 inhibits IKK with IC50 of 600 nM Homo sapiens N-(6-chloro-9H-beta-carbolin-8-yl)acetamide
0.0006
-
 inhibits IKK with IC50 of 600 nM Homo sapiens N-(6-chloro-9H-beta-carbolin-8-yl)-3-methoxybenzamide
0.0006
-
 inhibits IKK with IC50 of 600 nM Homo sapiens 5,6-dibromo-beta-carboline
0.0006
-
 inhibits IKK with IC50 of 600 nM Homo sapiens 5-bromo-6-chloro-beta-carboline
0.0007
-
 inhibits IKK with IC50 of 700 nM Homo sapiens N-(6-chloro-9H-beta-carbolin-8-yl)benzamide
0.0007
-
 inhibits IKK with IC50 of 700 nM Homo sapiens methyl (6-chloro-9H-beta-carbolin-8-yl)carbamate
0.001
-
 inhibits IKK with IC50 of 0.001 mM Homo sapiens N-(6-chloro-9H-beta-carbolin-8-yl)pyridine-2-carboxamide
0.0011
-
 inhibits IKK with IC50 of 0.0011 mM Homo sapiens 5-bromo-6-trifluoromethyl-beta-carboline
0.0011
-
 inhibits IKK with IC50 of 0.0011 mM Homo sapiens 5-bromo-6-cyano-beta-carboline
0.0013
-
 inhibits IKK with IC50 of 0.0013 mM Homo sapiens 8-amino-6-chloro-beta-carboline
0.0013
-
 inhibits IKK with IC50 of 0.0013 mM Homo sapiens N-(6-chloro-9H-beta-carbolin-8-yl)-4-methoxybenzamide
0.0018
-
 inhibits IKK with IC50 of 0.0018 mM Homo sapiens 8-methylamino-6-chloro-beta-carboline
0.0018
-
 inhibits IKK with IC50 of 0.0018 mM Homo sapiens 8-dimethylamino-6-chloro-beta-carboline
0.002
-
 inhibits IKK with IC50 of 0.002 mM Homo sapiens 5-bromo-6-fluoro-beta-carboline
0.003
-
 inhibits IKK with IC50 of 0.003 mM Homo sapiens N-(6-chloro-9H-beta-carbolin-8-yl)-2-(pyridin-2-yl)acetamide
0.003
-
 inhibits IKK with IC50 of 0.003 mM Homo sapiens 6,8-dichloro-7-(cyclohexylmethoxy)-9H-beta-carboline
0.0032
-
 inhibits IKK with IC50 of 0.0032 mM Homo sapiens 6,8-dichloro-9H-beta-carbolin-7-yl morpholine-4-carboxylate
0.004
-
 inhibits IKK with IC50 of 0.004 mM Homo sapiens 8-nitro-6-chloro-beta-carboline
0.004
-
 nonspecific inhibitor of IKK, inhibits IKK with IC50 of 0.004 mM Homo sapiens 5-bromo-6-methoxy-beta-carboline
0.0083
-
 inhibits IKK with IC50 of 0.0083 mM Homo sapiens N-(6-chloro-9H-beta-carbolin-8-yl)methanesulfonamide
0.011
-
 inhibits IKK with IC50 of 0.011 mM Homo sapiens 7-hydroxy-6,8-dichloro-beta-carboline
0.015
-
 inhibits IKK with IC50 of 0.015 mM Homo sapiens 5-bromo-beta-carboline
0.02
-
 inhibits IKK with IC50 of 0.02 mM Homo sapiens N-benzyl-6-chloro-9H-beta-carbolin-8-amine
0.02
-
 inhibits IKK with IC50 of 0.02 mM Homo sapiens N-(6-chloro-9H-beta-carbolin-8-yl)-4-hydroxybutanamide
0.02
-
 inhibits IKK with IC50 of 0.02 mM Homo sapiens N-(6-chloro-9H-beta-carbolin-8-yl)-2-methoxybenzamide
0.02
-
 inhibits IKK with IC50 of 0.02 mM Homo sapiens N-(6-chloro-9H-beta-carbolin-8-yl)benzenesulfonamide
0.02
-
 inhibits IKK with IC50 of 0.02 mM Homo sapiens 1-(6-chloro-9H-beta-carbolin-8-yl)-3-methylurea
0.02
-
 inhibits IKK with IC50 of 0.02 mM Homo sapiens N-(6-chloro-9H-beta-carbolin-8-yl)morpholine-4-carboxamide