UCF-101 (313649-08-0) is a potent, specific, competitive, and reversible inhibitor of the pro-apoptotic, mitochondrial serine protease Omi/HtrA2 (IC50 = 9.5 μM for His-Omi134-458). Shows very little activity against various other serine proteases tested (IC50 ≥ 200 μM).1 Mitigates streptozotocin-induced cardiomyocyte dysfunction.2 Protects against cerebral oxidative injury and cognitive impairment in a rat model.3 Cell permeable.
1) Cilenti et al. (2003), Characteristics of a novel and specific inhibitor for the pro-apoptotic protease Omi/HtrA2; J. Biol. Chem., 278 11489
2) Li et al. (2009), UCF-101 mitigates streptozotocin-induced cardiomyocyte dysfunction: role of AMPK; Am. J. Physiol. Endocrinol. Metab., 297 E965
3) Hu et al. (2013), Ucf-101 protects against cerebral oxidative injury and cognitive impairment in septic rat; Int. Immunopharmacol., 16 108