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Literature summary extracted from

  • Chew, E.H.; Lu, J.; Bradshaw, T.D.; Holmgren, A.
    Thioredoxin reductase inhibition by antitumor quinols: a quinol pharmacophore effect correlating to antiproliferative activity (2008), FASEB J., 22, 2072-2083.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.8.1.9 3-(4-[[2-(1-hydroxy-4-oxocyclohexa-2,5-dien-1-yl)-1H-indol-1-yl]sulfonyl]phenyl)propanoic acid
-
Rattus norvegicus
1.8.1.9 3-(4-[[6-fluoro-2-(1-hydroxy-4-oxocyclohexa-2,5-dien-1-yl)-1H-indol-1-yl]sulfonyl]phenyl)propanoic acid
-
Rattus norvegicus
1.8.1.9 4-(1,3-benzothiazol-2-yl)-4-hydroxycyclohexa-2,5-dien-1-one
-
Rattus norvegicus
1.8.1.9 4-(1,3-benzoxazol-2-yl)-4-hydroxycyclohexa-2,5-dien-1-one
-
Rattus norvegicus
1.8.1.9 4-(1-benzothien-2-yl)-4-hydroxycyclohexa-2,5-dien-1-one
-
Rattus norvegicus
1.8.1.9 4-(5-fluoro-1,3-benzothiazol-2-yl)-4-hydroxycyclohexa-2,5-dien-1-one
-
Rattus norvegicus
1.8.1.9 4-hydroxy-4-[1-(phenylsulfonyl)-1H-indol-2-yl]cyclohexa-2,5-dien-1-one
-
Rattus norvegicus
1.8.1.9 4-[6-fluoro-1-(phenylsulfonyl)-1H-indol-2-yl]-4-hydroxycyclohexa-2,5-dien-1-one
-
Rattus norvegicus
1.8.1.9 additional information quinols irreversible inhibit mammalian TrxR by targeting the penultimate C-terminal selenocysteine residue Rattus norvegicus

Organism

EC Number Organism UniProt Comment Textmining
1.8.1.9 Rattus norvegicus
-
recombinant
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.8.1.9 5,5'-dithiobis(2-nitrobenzoic acid) + NADPH + H+
-
Rattus norvegicus 2-nitro-5-thiobenzoate + NADP+
-
?
1.8.1.9 thioredoxin disulfide + NADPH + H+
-
Rattus norvegicus thioredoxin + NADP+
-
?

Synonyms

EC Number Synonyms Comment Organism
1.8.1.9 TrxR
-
Rattus norvegicus

Cofactor

EC Number Cofactor Comment Organism Structure
1.8.1.9 NADPH
-
Rattus norvegicus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.8.1.9 0.0027
-
pH 7.5, determined after 60 min incubation of recombinant rat TrxR with 5,5'-dithiobis(2-nitrobenzoic acid) as substrate, irreversible Rattus norvegicus 4-[6-fluoro-1-(phenylsulfonyl)-1H-indol-2-yl]-4-hydroxycyclohexa-2,5-dien-1-one
1.8.1.9 0.0029
-
pH 7.5, determined after 60 min incubation of recombinant rat TrxR with 5,5'-dithiobis(2-nitrobenzoic acid) as substrate, irreversible Rattus norvegicus 4-hydroxy-4-[1-(phenylsulfonyl)-1H-indol-2-yl]cyclohexa-2,5-dien-1-one
1.8.1.9 0.0063
-
pH 7.5, determined after 60 min incubation of recombinant rat TrxR with 5,5'-dithiobis(2-nitrobenzoic acid) as substrate, irreversible Rattus norvegicus 4-(5-fluoro-1,3-benzothiazol-2-yl)-4-hydroxycyclohexa-2,5-dien-1-one
1.8.1.9 0.0065
-
pH 7.5, determined after 60 min incubation of recombinant rat TrxR with 5,5'-dithiobis(2-nitrobenzoic acid) as substrate, irreversible Rattus norvegicus 4-(1,3-benzothiazol-2-yl)-4-hydroxycyclohexa-2,5-dien-1-one
1.8.1.9 0.0083
-
pH 7.5, determined after 60 min incubation of recombinant rat TrxR with 5,5'-dithiobis(2-nitrobenzoic acid) as substrate, irreversible Rattus norvegicus 3-(4-[[2-(1-hydroxy-4-oxocyclohexa-2,5-dien-1-yl)-1H-indol-1-yl]sulfonyl]phenyl)propanoic acid
1.8.1.9 0.0098
-
pH 7.5, determined after 60 min incubation of recombinant rat TrxR with 5,5'-dithiobis(2-nitrobenzoic acid) as substrate, irreversible Rattus norvegicus 3-(4-[[6-fluoro-2-(1-hydroxy-4-oxocyclohexa-2,5-dien-1-yl)-1H-indol-1-yl]sulfonyl]phenyl)propanoic acid
1.8.1.9 0.0761
-
pH 7.5, determined after 60 min incubation of recombinant rat TrxR with 5,5'-dithiobis(2-nitrobenzoic acid) as substrate, irreversible Rattus norvegicus 4-(1,3-benzoxazol-2-yl)-4-hydroxycyclohexa-2,5-dien-1-one
1.8.1.9 0.1043
-
pH 7.5, determined after 60 min incubation of recombinant rat TrxR with 5,5'-dithiobis(2-nitrobenzoic acid) as substrate, irreversible Rattus norvegicus 4-(1-benzothien-2-yl)-4-hydroxycyclohexa-2,5-dien-1-one