apaf-1

NS3694 is an inhibitor of apoptosis and inhibits apoptosome formation and caspase activation.

trans-Chalcone (Chalkone) is an aromatic ketone that forms the central core for a variety of important biological compounds, which are known collectively as chalcones.

QM31 is a selective Apaf-1 inhibitor(inbitita formation of the apoptosome with IC50 of 7.9μM).

ZYZ-488 is an Apoptotic Protease-Activating Factor 1 (Apaf-1) inhibitor that inhibits the activation of procaspase-9 and procaspase-3. It can be used to study cardiovascular diseases.

MDK83190 (Apoptosis Activator 2) is a potent apoptosis activator, induceing caspase-3 activation, PARP cleavage, and DNA fragmentation .

LPT-99 is an antagonist of the apoptosis protease-activating factor 1 (APAF-1). It inhibits the activation of procaspase-9 and can suppress apoptosis induced by Cisplatin. Additionally, LPT-99 effectively reduces Cisplatin-induced hearing loss in rats.

Mitochondrial release of cytochrome c triggers apoptosis via the assembly of a multimeric complex including caspase-9, Apaf-1, and other components, sometimes called the apoptosome. Library screens have identified small molecules that activate the apoptosome by binding to one or more of its components. CAY10443 is one such molecule. In a cell free, multi-component assay, it activated caspase-3 with an EC50 of 5 μM. These apoptotic activators represent therapeutic lead compounds for the development of antitumor drugs.

HA-14-1, a small molecule, binds the surface pocket of Bcl-2 proteins (IC50= ~ 9 µM), including Bcl-xl and Bcl-W, and disrupts their interaction with the Bak peptide. This action induces apoptosis by activating Apaf-1 and caspase-9 and -3. Additionally, HA-14-1 effectively induces apoptosis in human acute myeloid leukemia (HL-60) cells, with a 50 µM concentration resulting in a 90% loss of cell viability.

Cytochrome c fragment (93-108) is a peptide from Cytochrome c, which is a small heme protein found loosely associated with the inner membrane of the mitochondrion. Cytochromes c from certain eukaryotes, including plants and fungi but not higher animals, contains methylated lysine residues at specific positions1. Cytochrome c is a required cofactor for Apaf-1 function2.

Cytochrome P450 CYP1B1 (190-198) [Homo sapiens] is a peptide from Cytochrome c, which is a small heme protein found loosely associated with the inner membrane of the mitochondrion. Cytochromes c from certain eukaryotes, including plants and fungi but not higher animals, contains methylated lysine residues at specific positions1. Cytochrome c is a required cofactor for Apaf-1 function2.