Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(1,1-dihydroxy-3-oxo-1,3-dihydro-2H-1,2-benzisothiazol-2-yl)acetic acid | i.e. BiT, 1,1-dioxide-benzo[d]isothiazol-3-one alkanoic acid derivatives | Rattus norvegicus | |
(1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid | IC50: 0.010 mM | Rattus norvegicus | |
(1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid ethyl ester | - |
Rattus norvegicus | |
(1,3,3-trioxo-2,3-dihydronaphtho[2,3-d]isothiazol-2-yl)acetic acid ethyl ester | - |
Rattus norvegicus | |
(3,3-dihydroxy-1-oxo-1,3-dihydro-2H-3lambda4-naphtho[1,2-d]isothiazol-2-yl)acetic acid | i.e. NiT | Rattus norvegicus | |
(6-amino-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid | IC50: 0.10 mM | Rattus norvegicus | |
(6-amino-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid ethyl ester | - |
Rattus norvegicus | |
(6-nitro-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid | IC50: 0.180 mM | Rattus norvegicus | |
(6-nitro-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid ethyl ester | - |
Rattus norvegicus | |
(9-amino-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid | IC50: 0.10 mM | Rattus norvegicus | |
(9-amino-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid ethyl ester | - |
Rattus norvegicus | |
(9-nitro-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid | IC50: 0.190 mM | Rattus norvegicus | |
(9-nitro-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid ethyl ester | - |
Rattus norvegicus | |
1,1-dioxidenaphtho[2,3-d]isothiazole-3(2H)-one | - |
Rattus norvegicus | |
1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid | - |
Rattus norvegicus | |
2-benzyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid | IC50: 0.068 mM; IC50: 0.10 mM | Rattus norvegicus | |
2-benzyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid methyl ester | - |
Rattus norvegicus | |
2-carboxymethyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid | IC50: 140 nM, binding structure analysis | Rattus norvegicus | |
2-carboxymethyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid carboxymethyl ester | IC50: 550 nM, binding structure analysis | Rattus norvegicus | |
2-ethoxycarbonyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid ethoxycarbonylmethyl ester | - |
Rattus norvegicus | |
2-isopropoxycarbonylmethyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid isopropyl ester | - |
Rattus norvegicus | |
2-methyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid | IC50: 0.088 mM | Rattus norvegicus | |
2-methyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid ethoxycarbonyl methylester | - |
Rattus norvegicus | |
2-methyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid methyl ester | - |
Rattus norvegicus | |
2-tert-butylsulfonylnaphthalene-1,3-dicarboxylic acid | - |
Rattus norvegicus | |
2-tert-butylsulfonylnaphthalene-1-carboxylic acid | - |
Rattus norvegicus | |
3,3-dioxidenaphtho[1,2-d]isothiazole-1(2H)-one | - |
Rattus norvegicus | |
3-tert-butylsulfonylnaphthalene-2-carboxylic acid | - |
Rattus norvegicus | |
epalrestat | - |
Rattus norvegicus | |
additional information | inhibitor synthesis, overview, enzyme docking study, modeling, no inhibition by (1,3,3-trioxo-2,3-dihydronaphtho[2,3-d]isothiazol-2-yl)acetic acid and 2-methyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid | Rattus norvegicus | |
naphtho[1,2-d]isothiazole acetic acid derivatives | - |
Rattus norvegicus | |
sorbinil | - |
Rattus norvegicus | |
Tolrestat | - |
Rattus norvegicus | |
zopolrestat | - |
Rattus norvegicus |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Rattus norvegicus | P07943 | Sprague-Dawley rats | - |
Purification (Comment) | Organism |
---|---|
native enzyme partially from lens by ammonium sulfate fractionation and dialysis | Rattus norvegicus |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
lens | - |
Rattus norvegicus | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
DL-glyceraldehyde + NADPH + H+ | - |
Rattus norvegicus | glycerol + NADP+ | - |
? |
Synonyms | Comment | Organism |
---|---|---|
aldose reductase | - |
Rattus norvegicus |
ALR2 | - |
Rattus norvegicus |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
30 | - |
assay at | Rattus norvegicus |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
6.2 | - |
assay at | Rattus norvegicus |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
NADPH | - |
Rattus norvegicus |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00014 | - |
IC50: 140 nM, binding structure analysis | Rattus norvegicus | 2-carboxymethyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid | |
0.00055 | - |
IC50: 550 nM, binding structure analysis | Rattus norvegicus | 2-carboxymethyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid carboxymethyl ester | |
0.01 | - |
IC50: 0.010 mM | Rattus norvegicus | (1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid | |
0.068 | - |
IC50: 0.068 mM | Rattus norvegicus | 2-benzyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid | |
0.088 | - |
IC50: 0.088 mM | Rattus norvegicus | 2-methyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid | |
0.1 | - |
IC50: 0.10 mM | Rattus norvegicus | 2-benzyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid | |
0.1 | - |
IC50: 0.10 mM | Rattus norvegicus | (9-amino-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid | |
0.1 | - |
IC50: 0.10 mM | Rattus norvegicus | (6-amino-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid | |
0.18 | - |
IC50: 0.180 mM | Rattus norvegicus | (6-nitro-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid | |
0.19 | - |
IC50: 0.190 mM | Rattus norvegicus | (9-nitro-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid |