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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 cardioprotective property in significantly increasing the viability of hypoxia-induced H9c2 cardiomyocytes and reducing CK and LDH leakage, through interaction with Apaf-1 in procaspase-9 binding site. QM31 (SVT016426), a chemical inhibitor of Apaf-1, exerts mitochondria-protective functions while the direct interaction between QM31 and Apaf-1 was not clearly defined, decreases Cytc release and apoptosome-mediated activation of procaspase-9 preventing cell and tissue damage in ex vivo experiments and in vivo animal models of apoptotic damage.
 
Apaf-1 pharmacological inhibition has therapeutic potential for the treatment of apoptosis-related diseases.
 
 
 
References:
 
1. Wang Y, et al. The discovery of a novel inhibitor of apoptotic protease activating factor-1 (Apaf-1) for ischemic heart: synthesis, activity and target identification. Sci Rep. 2016 Jul 22;6:29820. doi: 10.1038/srep29820.
 
2. Malet G, et al. Small molecule inhibitors of Apaf-1-related caspase- 3/-9 activation that control mitochondrial-dependent apoptosis. Cell Death Differ. 2006 Sep;13(9):1523-32.
 
3. Imao T, et al. Apaf-1- and Caspase-8-independent apoptosis. Cell Death Differ. 2013 Feb;20(2):343-52. 
 
4. 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. doi: 10.1007/s10495-008-0310-x.
 
5. 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.

Cat. No. Product Name CAS No. Information
PC-62213

Leonurine

24697-74-3

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).

PC-35843

QM31

937735-00-7 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.
PC-62212

ZYZ-488

1470302-79-4 ZYZ-488 is a novel inhibitor of apoptotic protease activating factor-1 (Apaf-1), inhibits the activation of binding protein procaspase-9 and procaspase-3; exhibits cardioprotective effects on hypoxia-induced H9c2 rat ventricular cells, decreased apoptosis in hypoxic H9c2 cells, shows potential for treating cardiac ischemia.

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