Table 2.
Compound | Inhibition constant (μM) |
Mode of inhibition | |||
---|---|---|---|---|---|
IC50 | Kii | Kis | Comparison | ||
Zopolrestat | 9.0±0.6 | 11.0±0.5 | 12.5±0.5 | Kii≠Kis | mNC |
Fenofibrate | 10.0±0.5 | 11.5±0.5 | 16.5±0.6 | Kii≠Kis | mNC |
Wy 14,346 | 350.0±20.0 | 360.0±20.0 | 240.0±10.0 | Kii≠Kis | mNC |
Fenofibric acid | 220.0±15.0 | 250.0±10.0 | 240.0±10.0 | Kii≈Kis | pNC |
Gemfibrozil | 380.0±20.0 | 415.0±12.0 | 370.0±30.0 | Kii≠Kis | mNC |
Ciprofibrate | ND | 815.0±45.0 | 705.0±60.0 | Kii≠Kis | mNC |
mNC — mixed non-competitive; pNC — pure non-competitive; ND — not detectable; EBPC and sorbinil did not show measurable level of inhibiting C299S mutantAKR1B10.