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Literature summary for 1.8.1.9 extracted from

  • Yan, C.; Shieh, B.; Reigan, P.; Zhang, Z.; Colucci, M.A.; Chilloux, A.; Newsome, J.J.; Siegel, D.; Chan, D.; Moody, C.J.; Ross, D.
    Potent activity of indolequinones against human pancreatic cancer: identification of thioredoxin reductase as a potential target (2009), Mol. Pharmacol., 76, 163-172.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
medicine inhibition of thioredoxin reductase represents a potential target in pancreatic cancer and provides a biomarker of effect of lead indolequinones in this type of cancer Homo sapiens
medicine inhibition of thioredoxin reductase represents a potential target in pancreatic cancer and provides a biomarker of effect of lead indolequinones in this type of cancer Rattus norvegicus

Inhibitors

Inhibitors Comment Organism Structure
2-hydroxymethyl-5-methoxy-1-methyl-3-[(2,4,6-trifluorophenoxy)methyl]indole-4,7-dione maximum inhibition is achieved 5 min after addition of 0.003 mM Homo sapiens
2-hydroxymethyl-5-methoxy-1-methyl-3-[(2,4,6-trifluorophenoxy)methyl]indole-4,7-dione maximum inhibition is achieved 5 min after addition of 0.003 mM Rattus norvegicus
2-hydroxymethyl-5-methoxy-1-methyl-3-[(4-nitrophenoxy)methyl]indole-4,7-dione
-
Homo sapiens
2-hydroxymethyl-5-methoxy-1-methyl-3-[(4-nitrophenoxy)methyl]indole-4,7-dione
-
Rattus norvegicus
2-hydroxymethyl-6-methoxy-1-methyl-3-[(4-nitrophenoxy)methyl]indole-4,7-dione
-
Homo sapiens
2-hydroxymethyl-6-methoxy-1-methyl-3-[(4-nitrophenoxy)methyl]indole-4,7-dione
-
Rattus norvegicus
5-methoxy-1,2-dimethyl-3-[1-oxo-2-(2,4,6-trifluorophenyl)ethyl]indole-4,7-dione
-
Homo sapiens
5-methoxy-1,2-dimethyl-3-[1-oxo-2-(2,4,6-trifluorophenyl)ethyl]indole-4,7-dione
-
Rattus norvegicus
5-methoxy-1-methyl-3-[(2,4,6-trifluorophenoxy)methyl]indole-4,7-dione
-
Homo sapiens
5-methoxy-1-methyl-3-[(2,4,6-trifluorophenoxy)methyl]indole-4,7-dione
-
Rattus norvegicus
5-methoxy-1-methyl-3-[(4-nitrophenoxy)methyl]indole-4,7-dione
-
Homo sapiens
5-methoxy-1-methyl-3-[(4-nitrophenoxy)methyl]indole-4,7-dione
-
Rattus norvegicus
6-methoxy-1-methyl-3-[(2,4,6-trifluorophenoxy)methyl]indole-4,7-dione
-
Homo sapiens
6-methoxy-1-methyl-3-[(2,4,6-trifluorophenoxy)methyl]indole-4,7-dione
-
Rattus norvegicus
6-methoxy-1-methyl-3-[(4-nitrophenoxy)methyl]indole-4,7-dione
-
Homo sapiens
6-methoxy-1-methyl-3-[(4-nitrophenoxy)methyl]indole-4,7-dione
-
Rattus norvegicus
ES936 i.e. 5-methoxy-1,2-dimethyl-3-[(4-nitrophenoxy)methyl]indole-4,7-dione, potent inhibitor Homo sapiens
ES936 i.e. 5-methoxy-1,2-dimethyl-3-[(4-nitrophenoxy)methyl]indole-4,7-dione, potent inhibitor Rattus norvegicus

Organism

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

Source Tissue

Source Tissue Comment Organism Textmining
BxPC-3 cell
-
Homo sapiens
-
MiaPaCa-2 cell
-
Homo sapiens
-
additional information NCI-60 cell panel Homo sapiens
-
PANC-1 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5,5'-dithiobis(2-nitrobenzoic acid) + NADPH + H+
-
Homo sapiens 2-nitro-5-thiobenzoate + NADP+
-
?
5,5'-dithiobis(2-nitrobenzoic acid) + NADPH + H+
-
Rattus norvegicus 2-nitro-5-thiobenzoate + NADP+
-
?

Synonyms

Synonyms Comment Organism
thioredoxin reductase
-
Homo sapiens
thioredoxin reductase
-
Rattus norvegicus
TrxR
-
Homo sapiens
TrxR
-
Rattus norvegicus

Cofactor

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000082
-
in 100 mM potassium phosphate buffer, pH 7.4, at 22°C Rattus norvegicus 5-methoxy-1,2-dimethyl-3-[1-oxo-2-(2,4,6-trifluorophenyl)ethyl]indole-4,7-dione
0.000146
-
in 100 mM potassium phosphate buffer, pH 7.4, at 22°C Rattus norvegicus 2-hydroxymethyl-5-methoxy-1-methyl-3-[(2,4,6-trifluorophenoxy)methyl]indole-4,7-dione