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).1Mitigates streptozotocin-induced cardiomyocyte dysfunction.2Protects 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] LUCIA CILENTI. Characterization of a novel and specific inhibitor for the pro-apoptotic protease Omi/HtrA2.[J]. The Journal of Biological Chemistry, 2003, 278 13: 11489-11494. DOI:
10.1074/jbc.m212819200[2] QUN LI Jun R Ji Li. UCF-101 mitigates streptozotocin-induced cardiomyocyte dysfunction: role of AMPK.[J]. American journal of physiology. Endocrinology and metabolism, 2009, 297 4: E965-73. DOI:
10.1152/ajpendo.00323.2009[3] YUEYU HU . Ucf-101 protects against cerebral oxidative injury and cognitive impairment in septic rat[J]. International immunopharmacology, 2013, 16 1: Pages 108-113. DOI:
10.1016/j.intimp.2013.03.019
