Table 5.
Recently identified inhibitors of AKR1B10.
| Inhibitor * | IC50 (µM) ** | IC50 Ratio (1B10/1B1) |
References | |
|---|---|---|---|---|
| AKR1B10 | AKR1B1 | |||
| HCCFA | 0.0035 | 0.277 | 79 | [164] |
| HAHE | 0.0062 | 4.9 | 790 | [154] |
| MK204 | 0.080 | 21.7 | 271 | [165] |
| Oleanolic acid | 0.090 | 124 | 1370 | [155] |
| Epalrestat | 0.33 | 0.021 | 0.06 | [156] |
| Androst-3β,5α,6β,19-tetrol | 0.83 | >100 | 120 | [166] |
| Emodin | 0.99 | 12 | 12 | [157] |
| Arachidonic acid | 1.1 | 24 | 22 | [158] |
| Cohumulone | 1.35 | >125 | >93 | [159] |
| 8-Prenylnaringenin | 3.96 | 1.87 | 0.47 | [160] |
| Glycyrrhetinic acid | 4.9 | 280 | 57 | [156] |
Note: * Abbreviations: HCCFA, 7-hydroxy-2-oxo-2H-chromene-3-carboxylic acid [3-(4-fluorophenyl)propyl]amide; HAHE, 3-(4-hydroxy-2-methoxyphenyl)acrylic acid 3-(3-hydroxyphenyl)propyl ester; MK204, {5-chloro-2-[(pentabromobenzyl)carbamoyl]-phenoxy}acetic acid. ** IC50 value is determined with recombinant enzymes.