QM31 (SVT016426), a cytoprotective agent, is a selective inhibitor of Apaf-1. QM31 inhibits the formation of the apoptosome (IC50=7.9μM), the caspase activation complex composed by Apaf-1, cytochrome c, dATP and caspase-9. QM31 exerts mitochondrioprotective functions and interferes with the intra-S-phase DNA damage checkpoint[1][2].
SVT016426 (0.5-2 μM) inhibits Apaf1-induced activation of caspase activity with an IC50 of 5 μM in HeLa S100 cells[3].
[1]. MondragÓn L, et al. A chemical inhibitor of Apaf-1 exerts mitochondrioprotective functions and interferes with the intra-S-phase DNA damage checkpoint. Apoptosis. 2009 Feb;14(2):182-90.
[2]. OrzÁez M, et al. Apaf-1 inhibitors protect from unwanted cell death in in vivo models of kidney ischemia and chemotherapy induced ototoxicity. PLoS One. 2014 Oct 20;9(10):e110979.
[3]. Gortat A, et al. Apaf1 inhibition promotes cell recovery from apoptosis. Protein Cell. 2015 Nov;6(11):833-43.