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BV6 is a bivalent small-molecule Smac (Second Mitochondria-derived Activator of Caspases) mimetic that functions as a potent antagonist of Inhibitor of Apoptosis Proteins (IAPs), including cIAP1, cIAP2, and XIAP. By mimicking the N-terminal IAP-binding motif of mature Smac, BV6 induces the rapid proteasomal degradation of cIAPs and prevents XIAP from inhibiting caspases-3, -7, and -9. This action sensitizes cancer cells to apoptosis induced by death receptor ligands (such as TNFα or TRAIL) and various chemotherapeutic agents. BV6 is widely used as a pharmacological tool to study necroptosis and apoptosis pathways, particularly in the context of overcoming chemoresistance in malignancies such as glioblastoma, ovarian cancer, and leukemia.
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