Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(Z)-5-(naphthalen-1-ylmethylidene)-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione | 52% inhibition at 0.025 mM | Bos taurus | |
(Z)-5-(naphthalen-2-ylmethylidene)-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione | 59% inhibition at 0.025 mM | Bos taurus | |
(Z)-5-[(3-hydroxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione | - |
Bos taurus | |
(Z)-5-[(3-methoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione | - |
Bos taurus | |
(Z)-5-[(3-phenoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione | 64% inhibition at 0.025 mM | Bos taurus | |
(Z)-5-[(4-hydroxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione | - |
Bos taurus | |
(Z)-5-[(4-methoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione | - |
Bos taurus | |
(Z)-5-[(4-phenoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione | - |
Bos taurus | |
(Z)-5-[(4-phenylphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione | 45% inhibition at 0.025 mM | Bos taurus | |
epalrestat | - |
Bos taurus | |
fidarestat | - |
Bos taurus | |
lidorestat | - |
Bos taurus | |
additional information | synthesis and evaluation of 2,4-thiazolidinedione inhibitors, structure-activity relationships, overview. No inhibition by (Z)-5-[(4-benzyloxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione | Bos taurus | |
sorbinil | - |
Bos taurus | |
Tolrestat | - |
Bos taurus | |
zopolrestat | - |
Bos taurus |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Bos taurus | - |
- |
- |
Purification (Comment) | Organism |
---|---|
native enzyme from lens by anion exchange and Matrex Orange A affinity chromatography | Bos taurus |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
lens | - |
Bos taurus | - |
Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
---|---|---|---|
0.93 | - |
purified enzyme, pH 6.8, 37°C | Bos taurus |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
DL-glyceraldehyde + NADPH + H+ | - |
Bos taurus | DL-glycerol + NADP+ | - |
? |
Synonyms | Comment | Organism |
---|---|---|
aldose reductase | - |
Bos taurus |
ALR2 | - |
Bos taurus |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Bos taurus |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
6.8 | - |
assay at | Bos taurus |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
NADPH | - |
Bos taurus |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.002 | - |
pH 6.8, 37°C | Bos taurus | sorbinil | |
0.003 | - |
pH 6.8, 37°C | Bos taurus | (Z)-5-[(4-hydroxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione | |
0.0083 | - |
pH 6.8, 37°C | Bos taurus | (Z)-5-[(4-phenoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione | |
0.0123 | - |
pH 6.8, 37°C | Bos taurus | (Z)-5-[(3-hydroxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione | |
0.0174 | - |
pH 6.8, 37°C | Bos taurus | (Z)-5-[(4-methoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione | |
0.0233 | - |
pH 6.8, 37°C | Bos taurus | (Z)-5-[(3-methoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione |