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Literature summary for 2.7.11.24 extracted from

  • De, S.K.; Chen, L.H.; Stebbins, J.L.; Machleidt, T.; Riel-Mehan, M.; Dahl, R.; Chen, V.; Yuan, H.; Barile, E.; Emdadi, A.; Murphy, R.; Pellecchia, M.
    Discovery of 2-(5-nitrothiazol-2-ylthio)benzo[d]thiazoles as novel c-Jun N-terminal kinase inhibitors (2009), Bioorg. Med. Chem., 17, 2712-2717.
    View publication on PubMedView publication on EuropePMC

Activating Compound

Activating Compound Comment Organism Structure
additional information activated by a range of stress stimuli, such as heat shock, irradiation, hypoxia, chemotoxins, and peroxides, also activated in response to various cytokines Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-methyl-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-benzimidazole
-
Homo sapiens
2,2'-disulfanediylbis(1,3-benzothiazole)
-
Homo sapiens
2-[(2,4-dinitrophenyl)sulfanyl]-1,3-benzoxazole
-
Homo sapiens
2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzothiazole
-
Homo sapiens
2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzoxazole
-
Homo sapiens
2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-benzimidazole
-
Homo sapiens
2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-benzimidazole-5-sulfonic acid
-
Homo sapiens
2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-5-(trifluoromethyl)-1H-benzimidazole
-
Homo sapiens
2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl][1,3]thiazolo[4,5-b]pyridine
-
Homo sapiens
4-[(1H-benzimidazol-2-ylsulfanyl)methyl]benzoic acid
-
Homo sapiens
4-[[(6-amino-9H-purin-8-yl)sulfanyl]methyl]benzoic acid
-
Homo sapiens
5,6-dichloro-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-benzimidazole
-
Homo sapiens
5-chloro-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzothiazole
-
Homo sapiens
5-chloro-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzoxazole
-
Homo sapiens
5-methoxy-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzothiazole
-
Homo sapiens
5-methoxy-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-benzimidazole
-
Homo sapiens
5-methyl-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-benzimidazole
-
Homo sapiens
5-nitro-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-benzimidazole
-
Homo sapiens
6-chloro-2-[(4-methyl-5-thiophen-2-yl-4H-1,2,4-triazol-3-yl)sulfanyl]-1,3-benzothiazole
-
Homo sapiens
6-chloro-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzothiazole
-
Homo sapiens
6-chloro-2-[[4-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-methyl-4H-1,2,4-triazol-3-yl]sulfanyl]-1,3-benzothiazole
-
Homo sapiens
6-chloro-2-[[5-(2,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]sulfanyl]-1,3-benzothiazole
-
Homo sapiens
6-chloro-2-[[5-(2-methoxyphenyl)-4-phenyl-4H-1,2,4-triazol-3-yl]sulfanyl]-1,3-benzothiazole
-
Homo sapiens
6-ethoxy-1,3-benzothiazole-2-sulfonamide
-
Homo sapiens
6-ethoxy-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzothiazole
-
Homo sapiens
6-methyl-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzoxazole
-
Homo sapiens
6-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-9H-purin-2-amine
-
Homo sapiens
6-[5-[(6-chloro-1,3-benzothiazol-2-yl)sulfanyl]-4-methyl-4H-1,2,4-triazol-3-yl]quinoline
-
Homo sapiens
8-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-9H-purin-6-amine
-
Homo sapiens
pep-JIP1 peptide corresponding to the D-domain of JIP-1, final sequence of the most extensively used peptide is GRKKRRQRRRPPRPKRPTTLNLFPQVPRSQDT Homo sapiens
S-1,3-benzothiazol-2-yl (2Z)-(2-amino-1,3-thiazol-4-yl)(methoxyimino)ethanethioate
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + a protein Homo sapiens
-
ADP + a phosphoprotein
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HeLa cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + a protein
-
Homo sapiens ADP + a phosphoprotein
-
?
ATP + ATF2 substrate in in vitro kinase assay, LanthaScreen Homo sapiens ADP + phosphorylated ATF2
-
?
ATP + c-Jun transcription factor JNK phosphorylates the N-terminal transactivation domain of c-Jun transcription factor Homo sapiens ADP + phosphorylated c-Jun transcription factor
-
?

Synonyms

Synonyms Comment Organism
c-Jun N-terminal kinase
-
Homo sapiens
JNK
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0018
-
-
Homo sapiens 2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzothiazole
0.0018
-
-
Homo sapiens 5-methoxy-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzothiazole
0.0027
-
-
Homo sapiens 2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzoxazole
0.0038
-
-
Homo sapiens 5-methyl-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-benzimidazole
0.0042
-
-
Homo sapiens 2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl][1,3]thiazolo[4,5-b]pyridine
0.0047
-
-
Homo sapiens 5-methoxy-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-benzimidazole
0.0064
-
-
Homo sapiens 5-nitro-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-benzimidazole
0.0081
-
-
Homo sapiens 2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-benzimidazole
0.0202
-
-
Homo sapiens 2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-5-(trifluoromethyl)-1H-benzimidazole
0.023
-
-
Homo sapiens 5,6-dichloro-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-benzimidazole
0.027
-
-
Homo sapiens 5-chloro-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzoxazole
0.027
-
-
Homo sapiens 8-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-9H-purin-6-amine
0.05
-
-
Homo sapiens 2,2'-disulfanediylbis(1,3-benzothiazole)
0.05
-
larger than 0.050 Homo sapiens 6-ethoxy-1,3-benzothiazole-2-sulfonamide
0.05
-
larger than 0.050 Homo sapiens 1-methyl-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-benzimidazole
0.05
-
larger than 0.050 Homo sapiens 2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-benzimidazole-5-sulfonic acid
0.05
-
larger than 0.050 Homo sapiens 5-chloro-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzothiazole
0.05
-
larger than 0.050 Homo sapiens 6-chloro-2-[(4-methyl-5-thiophen-2-yl-4H-1,2,4-triazol-3-yl)sulfanyl]-1,3-benzothiazole
0.05
-
larger than 0.050 Homo sapiens 6-chloro-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzothiazole
0.05
-
larger than 0.050 Homo sapiens 6-chloro-2-[[4-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-methyl-4H-1,2,4-triazol-3-yl]sulfanyl]-1,3-benzothiazole
0.05
-
larger than 0.050 Homo sapiens 6-chloro-2-[[5-(2,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]sulfanyl]-1,3-benzothiazole
0.05
-
larger than 0.050 Homo sapiens 6-chloro-2-[[5-(2-methoxyphenyl)-4-phenyl-4H-1,2,4-triazol-3-yl]sulfanyl]-1,3-benzothiazole
0.05
-
larger than 0.050 Homo sapiens 6-ethoxy-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzothiazole
0.05
-
larger than 0.050 Homo sapiens 6-methyl-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzoxazole
0.05
-
larger than 0.050 Homo sapiens 6-[5-[(6-chloro-1,3-benzothiazol-2-yl)sulfanyl]-4-methyl-4H-1,2,4-triazol-3-yl]quinoline
0.05
-
larger than 0.050 Homo sapiens S-1,3-benzothiazol-2-yl (2Z)-(2-amino-1,3-thiazol-4-yl)(methoxyimino)ethanethioate
0.055
-
-
Homo sapiens 6-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-9H-purin-2-amine
0.07
-
-
Homo sapiens 4-[[(6-amino-9H-purin-8-yl)sulfanyl]methyl]benzoic acid
0.1
-
larger than 0.100 Homo sapiens 2-[(2,4-dinitrophenyl)sulfanyl]-1,3-benzoxazole
0.1
-
larger than 0.100 Homo sapiens 4-[(1H-benzimidazol-2-ylsulfanyl)methyl]benzoic acid

Expression

Organism Comment Expression
Homo sapiens up-regulation of JNK activity is associated with a number of disease states such as type-2 diabetes, obesity, cancer, inflammation, and stroke up