UCF-101 is a specific inhibitor for the pro-apoptotic protease Omi/HtrA2 with IC50 of 9.5 uM, displays high selectivity over other serine proteases. UCF-101 restores heart dysfunction following ischemia/reperfusion injury in vivo. UCF-101 prevented loss of membrane integrity by inhibiting fodrin breakdown in cardiomyocytes. UCF-101 rescues cardiomyocytes from ischemia/reperfusion injury by inhibiting XIAP degradation and Fas/Fas-ligand-induced apoptosis, thereby ameliorating ischemia/reperfusion-induced myocardial dysfunction.
