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Literature summary for 1.8.1.9 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
Search for more literature for 1.8.1.9

Inhibitors

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

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
 recombinant
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
TrxR
-
 Rattus norvegicus

Cofactor

Cofactor Comment Organism Structure
NADPH
-
 Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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
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
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
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
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
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
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
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