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Literature summary extracted from

  • Yee, D.J.; Balsanek, V.; Bauman, D.R.; Penning, T.M.; Sames, D.
    Fluorogenic metabolic probes for direct activity readout of redox enzymes: Selective measurement of human AKR1C2 in living cells (2006), Proc. Natl. Acad. Sci. USA, 103, 13304-13309.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.1.1.50 expression in Cos-1 cells Homo sapiens
1.1.1.213 expression in Cos-1 cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.50 9-(phenylcarbonyl)-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one competitive Homo sapiens
1.1.1.50 celecoxib synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.050 mM in fluorometric assay, in vitro IC50: 0.050 mM in fluorometric assay Homo sapiens
1.1.1.50 Flufenamic acid synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.0040 mM in fluorometric assay, in vitro IC50: 0.00031 mM in fluorometric assay Homo sapiens
1.1.1.50 Ibuprofen synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.017 mM in fluorometric assay, in vitro IC50: 0.009 mM in fluorometric assay Homo sapiens
1.1.1.50 naproxen synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.0094 mM in fluorometric assay, 0.016 mM in radiometric assay, in vitro IC50: 0.0027 mM in fluorometric assay Homo sapiens
1.1.1.50 ursodeoxycholate natural inhibitor, in vivo IC50: 0.00024 mM in fluorometric assay, 0.00014 mM in radiometric assay, in vitro IC50: 0.000049 mM in fluorometric assay Homo sapiens
1.1.1.213 9-(phenylcarbonyl)-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one competitive Homo sapiens
1.1.1.213 celecoxib synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.050 mM in fluorometric assay, in vitro IC50: 0.050 mM in fluorometric assay Homo sapiens
1.1.1.213 Flufenamic acid synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.0040 mM in fluorometric assay, in vitro IC50: 0.00031 mM in fluorometric assay Homo sapiens
1.1.1.213 Ibuprofen synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.017 mM in fluorometric assay, in vitro IC50: 0.009 mM in fluorometric assay Homo sapiens
1.1.1.213 naproxen synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.0094 mM in fluorometric assay, 0.016 mM in radiometric assay, in vitro IC50: 0.0027 mM in fluorometric assay Homo sapiens
1.1.1.213 ursodeoxycholate natural inhibitor, in vivo IC50: 0.00024 mM in fluorometric assay, 0.00014 mM in radiometric assay, in vitro IC50: 0.000049 mM in fluorometric assay Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.1.1.50 0.0013
-
5alpha-dihydrotestosterone recombinant enzyme in intact COS-1 cells Homo sapiens
1.1.1.50 0.003
-
9-(phenylcarbonyl)-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one recombinant enzyme in intact COS-1 cells Homo sapiens
1.1.1.213 0.0013
-
5alpha-dihydrotestosterone recombinant enzyme in intact COS-1 cells Homo sapiens
1.1.1.213 0.003
-
9-(phenylcarbonyl)-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one recombinant enzyme in intact COS-1 cells Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.1.1.50 5alpha-dihydrotestosterone + NADPH + H+ Homo sapiens inactivation of the potent androgen in human prostate, fluorometric activity measurement in intact cells, overview 5alpha-androstan-3alpha,17beta-diol + NADP+
-
?
1.1.1.50 9-(phenylcarbonyl)-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one + NADPH Homo sapiens competitive substrate, fluorometric activity measurement in intact cells, overview 9-[hydroxy(phenyl)methyl]-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one + NADP+
-
?
1.1.1.213 5alpha-dihydrotestosterone + NADPH + H+ Homo sapiens inactivation of the potent androgen in human prostate, fluorometric activity measurement in intact cells, overview 5alpha-androstan-3alpha,17beta-diol + NADP+
-
?
1.1.1.213 9-(phenylcarbonyl)-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one + NADPH Homo sapiens competitive substrate, fluorometric activity measurement in intact cells, overview 9-[hydroxy(phenyl)methyl]-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one + NADP+
-
?

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.50 Homo sapiens
-
-
-
1.1.1.213 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.1.1.50 prostate
-
Homo sapiens
-
1.1.1.213 prostate gland
-
Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.50 5alpha-dihydrotestosterone + NADPH + H+ inactivation of the potent androgen in human prostate, fluorometric activity measurement in intact cells, overview Homo sapiens 5alpha-androstan-3alpha,17beta-diol + NADP+
-
?
1.1.1.50 5alpha-dihydrotestosterone + NADPH + H+ i.e. DHT Homo sapiens 5alpha-androstan-3alpha,17beta-diol + NADP+
-
?
1.1.1.50 9-(phenylcarbonyl)-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one + NADPH competitive substrate, fluorometric activity measurement in intact cells, overview Homo sapiens 9-[hydroxy(phenyl)methyl]-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one + NADP+
-
?
1.1.1.50 9-(phenylcarbonyl)-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one + NADPH competitive substrate Homo sapiens 9-[hydroxy(phenyl)methyl]-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one + NADP+
-
?
1.1.1.213 5alpha-dihydrotestosterone + NADPH + H+ inactivation of the potent androgen in human prostate, fluorometric activity measurement in intact cells, overview Homo sapiens 5alpha-androstan-3alpha,17beta-diol + NADP+
-
?
1.1.1.213 5alpha-dihydrotestosterone + NADPH + H+ i.e. DHT Homo sapiens 5alpha-androstan-3alpha,17beta-diol + NADP+
-
?
1.1.1.213 9-(phenylcarbonyl)-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one + NADPH competitive substrate, fluorometric activity measurement in intact cells, overview Homo sapiens 9-[hydroxy(phenyl)methyl]-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one + NADP+
-
?
1.1.1.213 9-(phenylcarbonyl)-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one + NADPH competitive substrate Homo sapiens 9-[hydroxy(phenyl)methyl]-2,3,6,7-tetrahydro-1H,5H,11H-pyrano[2,3-f]pyrido[3,2,1-ij]quinolin-11-one + NADP+
-
?

Synonyms

EC Number Synonyms Comment Organism
1.1.1.50 AKR1C2
-
Homo sapiens
1.1.1.50 More cf. EC 1.1.1.213, the enzyme belongs to the aldo-keto reductase, AKR, superfamily Homo sapiens
1.1.1.213 AKR1C2
-
Homo sapiens
1.1.1.213 More cf. EC 1.1.1.50, the enzyme belongs to the aldo-keto reductase, AKR, superfamily Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.50 NADPH
-
Homo sapiens
1.1.1.213 NADPH
-
Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.50 0.000049
-
natural inhibitor, in vivo IC50: 0.00024 mM in fluorometric assay, 0.00014 mM in radiometric assay, in vitro IC50: 0.000049 mM in fluorometric assay Homo sapiens ursodeoxycholate
1.1.1.50 0.00031
-
synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.0040 mM in fluorometric assay, in vitro IC50: 0.00031 mM in fluorometric assay Homo sapiens Flufenamic acid
1.1.1.50 0.0027
-
synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.0094 mM in fluorometric assay, 0.016 mM in radiometric assay, in vitro IC50: 0.0027 mM in fluorometric assay Homo sapiens naproxen
1.1.1.50 0.009
-
synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.017 mM in fluorometric assay, in vitro IC50: 0.009 mM in fluorometric assay Homo sapiens Ibuprofen
1.1.1.50 0.05
-
synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.050 mM in fluorometric assay, in vitro IC50: 0.050 mM in fluorometric assay Homo sapiens celecoxib
1.1.1.213 0.000049
-
natural inhibitor, in vivo IC50: 0.00024 mM in fluorometric assay, 0.00014 mM in radiometric assay, in vitro IC50: 0.000049 mM in fluorometric assay Homo sapiens ursodeoxycholate
1.1.1.213 0.00031
-
synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.0040 mM in fluorometric assay, in vitro IC50: 0.00031 mM in fluorometric assay Homo sapiens Flufenamic acid
1.1.1.213 0.0027
-
synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.0094 mM in fluorometric assay, 0.016 mM in radiometric assay, in vitro IC50: 0.0027 mM in fluorometric assay Homo sapiens naproxen
1.1.1.213 0.009
-
synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.017 mM in fluorometric assay, in vitro IC50: 0.009 mM in fluorometric assay Homo sapiens Ibuprofen
1.1.1.213 0.05
-
synthetic, nonsteroidal anti-inflammatory inhibitor, in vivo IC50: 0.050 mM in fluorometric assay, in vitro IC50: 0.050 mM in fluorometric assay Homo sapiens celecoxib