Q-VD-OPH is a broad-spectrum caspase inhibitor, blocking caspases-3, -7, -8, -9, -10, and -12 and inhibiting apoptosis when used at 10 μM. It more effectively inhibits apoptosis and is much less cytotoxic than Z-VAD-FMK and Boc-D-FMK . Q-VD-OPH can be used in vivo, where it has been shown to prevent ischemia-reperfusion injury-induced apoptosis. This compound, by broadly inhibiting caspases, also promotes the differentiation of leukemic blasts cells, suggesting an application in differentiation therapy of certain forms of cancer.
An inhibitor that is used in Alzheimer’s studies relating to caspase-6, the cysteinyl protease involved in neurodegenerative conditions. As well it is an intermediate in the formation of Palinavir, a potent HIV protease inhibitor.
Q-VD-OPh hydrate has been used:
- as a pan-caspase inhibitor to prevent cell death in urothelial carcinoma cells (UCC)
- to induce canonical caspase-dependent apoptosis in UC cells
- to block caspase-3 and Poly (ADP-ribose) polymerase-1 (PARP-1)
- to study the protective role of EspZ effector protein against apoptosis and necrosis in human epithelial cells
Q-VD-OPh is a potent pan-caspase inhibitor that protects cells from capsase-dependent apoptosis. Q-VD-OPh has superior aqueous stability, cell permeability, and efficacy than FMK-based caspase inhibitors and displays no cytotoxic effects alone.
1) Caserta?et al.?(2003),?Q-VD-OPh, a broad spectrum caspase inhibitor with potent antiapoptotic properties; Apoptosis,?8?345
2) Braun?et al.?(2007),?Protection from brain damage and bacterial infection in murine stroke by the novel caspase-inhibitor Q-VD-OPH; Exp. Neurol.,?206?183
3) Rebbaa?et al.?(2003),?Caspase inhibition switches doxorubicin-induced apoptosis to senescence; Oncogene,?22?2805
4) Bulatovic?et al.?(2015),?Sublethal caspase activation promotes generation of cardiomyocytes from embryonic stem cells; PLoS One,?10?e0120176
5) Bailey?et al. (2017),?Augmented trophoblast cell death in preeclampsia can proceed via ceramide-mediated necroptosis;?Cell Death Dis.,?8?e2590
