Venetoclax

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Venetoclax (CAS-RN 1257044-40-8) is an antineoplastic agent approved in 2016 by US FDA to treat patients with Chronic Lymphocytic Leukemia (CLL). Venetoclax is a potent and selective inhibitor of the antiapoptotic protein BCL-2 (B-cell lymphoma). It binds directly to the binding site of the BH3 domain of BCL-2 and thereby displaces propoptotic proteins with BH3 domains, such as BIM, to initiate permeabilization of the mitochondrial outer membrane (MOMP), caspase activation and programmed cell death.