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. Author manuscript; available in PMC: 2018 Oct 18.
Published in final edited form as: Eur J Pharmacol. 2008 Feb 5;584(2-3):213–221. doi: 10.1016/j.ejphar.2008.01.036

Table 2.

Inhibition kinetic parameters for DL-glyceraldehyde reduction activity of C299S mutant AKR1B10 by various inhibitors

Compound Inhibition constant (μM)
Mode of inhibition
IC50 Kii Kis Comparison
Zopolrestat 9.0±0.6 11.0±0.5 12.5±0.5 KiiKis mNC
Fenofibrate 10.0±0.5 11.5±0.5 16.5±0.6 KiiKis mNC
Wy 14,346 350.0±20.0 360.0±20.0 240.0±10.0 KiiKis mNC
Fenofibric acid 220.0±15.0 250.0±10.0 240.0±10.0 KiiKis pNC
Gemfibrozil 380.0±20.0 415.0±12.0 370.0±30.0 KiiKis mNC
Ciprofibrate ND 815.0±45.0 705.0±60.0 KiiKis mNC

mNC — mixed non-competitive; pNC — pure non-competitive; ND — not detectable; EBPC and sorbinil did not show measurable level of inhibiting C299S mutantAKR1B10.