MV1

MV1 is a monovalent small molecule antagonist of the inhibitor of apoptosis protein (IAP) family, originally developed by Genentech. It binds with high affinity to the BIR3 domains of cellular IAP 1 (cIAP1), cellular IAP 2 (cIAP2), and X-linked inhibitor of apoptosis protein (XIAP), with Kd values of 6.0 nM for cIAP1-BIR3 and 16.0 nM for XIAP-BIR3. By mimicking the N-terminal IAP-binding motif of the endogenous protein SMAC/DIABLO, MV1 induces the autoubiquitination and rapid proteasomal degradation of cIAP1 and cIAP2, thereby promoting TNF-alpha-dependent apoptosis in cancer cells. In addition to its role as a direct apoptotic agent, MV1 is widely utilized in chemical biology as an E3 ligase-recruiting warhead in targeted protein degradation (TPD) systems, such as Specific and Nongenetic IAP-dependent Protein Erasers (SNIPERs) and PROTACs, as well as in HaloTag-based protein knockdown systems.

Other names

MV-1MV1MV 1