Comparison of inhibitor sensitivity among AKRs (AKR1C30, AKR1C31, AKR1C32, and AKR1C33)
| Inhibitor | AKR1C30 | AKR1C31 | AKR1C32 | AKR1C33 | ||||
|---|---|---|---|---|---|---|---|---|
| IC50 | Ki | IC50 | Ki | IC50 | Ki | IC50 | Ki | |
| μM | nM | μM | nM | μM | nM | μM | nM | |
| AKR1C30-selective type | ||||||||
| Carbenoxolone | 7.2 ± 1.0 | 840 ± 25 | >50 | >50 | >50 | |||
| Valproic acid | 40 ± 8 | 6200 ± 100 | >1000 | 450 ± 50 | >1000 | |||
| Phenobarbital | 1100 ± 120 | 64,000 ± 900 | >2000 | >2000 | >2000 | |||
| AKR1C31-selective type | ||||||||
| Baccharin | 12 ± 1.0 | 0.057 ± 0.005 | 6.0 ± 0.1 | >50 | 50 ± 6 | |||
| 7-Hydroxyflavone | 2.5 ± 1.0 | 0.059 ± 0.009 | 6.9 ± 0.2 | 1.1 ± 0.2 | 4.5 ± 0.3 | |||
| AKR1C32-selective | ||||||||
| Phenolphthalein | 0.97 ± 0.03 | 1.5 ± 0.1 | 0.021 ± 0.002 | 2.1 ± 0.3 | 12 ± 2 | |||
| Hinokitiol | 7.2 ± 0.2 | 12 ± 1 | 0.72 ± 0.08 | 100 ± 11 | >50 | |||
| AKR1C33-selective type | ||||||||
| Hexestrol | 7.0 ± 0.2 | 6.4 ± 0.8 | 9.8 ± 0.3 | 0.19 ± 0.2 | 17 ± 2 | |||
| Zearalenone | >20 | >20 | >20 | 0.22 ± 0.02 | 18 ± 3 | |||
| Diethylstilbestrol | 9.9 ± 0.5 | 8.2 ± 0.3 | 21 ± 2 | 0.24 ± 0.03 | 19 ± 2 | |||
| Betamethasone | >50 | >50 | >50 | 8.9 ± 0.5 | ||||
| Nonspecific type | ||||||||
| Isolithocholic acid | 0.23 ± 0.02 | 28 ± 3 | >50 | 6.5 ± 0.2 | 1.2 ± 0.1 | |||
| Kaempferol | 1.8 ± 0.2 | 0.33 ± 0.03 | 1.4 ± 0.2 | 0.37 ± 0.04 | ||||
| Quercetin | 2.3 ± 0.3 | 3.4 ± 0.4 | 5.2 ± 0.5 | 0.87 ± 0.09 | ||||
| Flufenamic acid | 24 ± 3 | 7.9 ± 0.9 | 44 ± 8 | 17 ± 3 | ||||