Description
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.
Uses
UCF 101 is a specific inhibitor of Omi/HtrA2, a proapoptotic mitochondrial serine protease. UCF 101 has the neuroprotective effects on cerebral oxidative injury and cognitive impairment in septic rats.
in vitro
ucf 101 was identified in a hts of a combinatorial library using omi-(134-458) protease and fluorescein-casein as a generic substrate. ucf 101 exhibited specific activity against omi/htra2 and very little activity against other serine proteases. ucf 101 showed a natural fluorescence that was used to monitor its ability to enter mammalian cells. in addition, when tested in caspase-9 (-/-) null fibroblasts, ucf 101 was able to inhibit omi/htra2-induced cell death [1].
in vivo
in a previous study, rats were intraperitoneally administered ucf-101 at 1.5 micromol/kg 10 min prior to reperfusion. results showed that ucf-101 treatment could significantly decrease cerebral infarct size by about 16.27% and also improve neurological behavior. moreover, ucf-101 treatment was able to reduce tunel-positive cells in the cerebral cortex significantly. in addition, the upregulation in the expression of fasl and the cleavage products of active caspase-3 and caspase-8 induced by ischemia was attenuated in mice treated with ucf-101, while upregulation of flip levels was increased [2].
References
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
