Table 2.
Compound | Inhibition constant (μM) |
Mode of inhibition | ||
---|---|---|---|---|
IC50 | Kii | Kis | ||
Ciprofibrate | ND | 815 | 705 | mNC |
Fenofibrate | 10 | 11 | 16 | mNC |
Fenofibric acid | 220 | 250 | 240 | pNC |
Gemfibrozil | 380 | 415 | 370 | mNC |
Wy 14,346 | 350 | 360 | 240 | mNC |
Zopolrestat | 9 | 11 | 12 | mNC |
mNC–mixed non-competitive; pNC–pure non-competitive; ND–not detectable; EBPC and sorbinil did not show measurable levels of inhibiting Cys299Ser mutant AKR1B10.