SM-1295 是凋亡蛋白 IAP 的拮抗剂，其对 XIAP-BIR3、c-IAP1-BIR3 和 c-IAP2-BIR3 的 Kd 值分别为 3077 nM、3.2 nM 和 9.5 nM。
SM-1295 is an inhibitor of apoptosis protein (IAP) antagonist, with Kd values of 3077 nM, 3.2 nM and 9.5 nM for XIAP-BIR3, c-IAP1-BIR3 and c-IAP2-BIR3, respectively[1][2].
SM-1295 (compound 5) binds to both cIAP1 and cIAP2 proteins with Ki values of 900-fold for cIAP1 over XIAP[1].SM-1295 (compound 5) exhibits an IC50 of 46 nM in MDA-MB-231[1].
[1]. Haiying Sun, et al. Potent and Selective Small-Molecule Inhibitors of cIAP1/2 Proteins Reveal That the Binding of Smac Mimetics to XIAP BIR3 Is Not Required for Their Effective Induction of Cell Death in Tumor Cells. ACS Chem Biol. 2014 Apr 18;9(4):994-1002.
[2]. Hui Cong, et al. Inhibitor of Apoptosis Protein (IAP) Antagonists in Anticancer Agent Discovery: Current Status and Perspectives. J Med Chem. 2019 Jun 27;62(12):5750-5772.
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