SM-164是一种有效的细胞通透性Smac类似物,能与XIAP蛋白结合(Ki=0.56 nM),并与cIAP-1和cIAP-2蛋白结合,Ki分别为0.31和1.1 nM。SM-164拮抗XIAP,诱导完全的cIAP-1降解,并诱导TNF-alpha依赖的肿瘤细胞凋亡。在MDA-MB-231移植瘤小鼠中,SM-164有效降解cIAP-1水平,并诱导肿瘤细胞凋亡,引起肿瘤衰退,但对正常小鼠组织没有毒性。
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参考文献
[1] Zhang S, et al. Smac mimetic SM-164 potentiates APO2L/TRAIL- and doxorubicin-mediated anticancer activity in human hepatocellular carcinoma cells. PLoS One. 7(12): e51461 (2012).
[2] Lu J, et al. SM-164: a novel, bivalent Smac mimetic that induces apoptosis and tumor regression by concurrent removal of the blockade of cIAP-1/2 and XIAP. Cancer Res. 68(22):9384-9393 (2008).
[3] Yang J, et al. Radiosensitization of head and neck squamous cell carcinoma by a SMAC-mimetic compound, SM-164, requires activation of caspases. Mol Cancer Ther. 10(4): 658-669 (2011).
冰袋运输。粉末直接保存于-20 ºC,有效期2年。溶于DMSO。建议分装后-20ºC避光保存,避免反复冻存,至少可存放6个月。