Apaf-1 is a central component in the apoptosis regulatory network for the treatment of apoptosis related diseases. Excessive Apaf-1 activity induced by myocardial ischemia causes cell injury. A novel compound, ZYZ-488, exhibited significant cardiopro
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QM31 (SVT016426, Apaf-1 inhibitor QM31) is a cytoprotective agent that inhibits the formation of the apoptosome (IC50=7.9 uM in vitro), the caspase activation complex composed by Apaf-1, cytochrome c, dATP and caspase-9; suppresses the Apaf-1-dependent intra-S-phase DNA damage checkpoint; QM31 can interfere with the two known functions of Apaf-1, namely apoptosome assembly/activation and intra-S-phase cell cycle arrest.
Leonurine (SCM-198) is a natural alkaloid that exhibits cardio-and neuronal-protective effects both in vitro and in vivo, occupies the caspase recruitment site of Apaf-1, blocks its interaction with procaspase-9; attenuates doxorubicin-induced apoptosis in H9c2 cardiac muscle cells, protects middle cerebral artery occluded rats through antioxidant effect and regulation of mitochondrial function, attenuates myocardial fibrotic response via inhibition of NADPH oxidase 4 (Nox4).
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