IAP antagonist; binds to the BIR3 domain of cIAP1, cIAP2 and XIAP with nanomolar affinity. Reduces cIAP1, cIAP2 and XIAP protein levels in human breast cancer MDA-MB-231 cells. Induces apoptosis in combination with TNF, and potentiates TRAIL-mediated apoptosis in human colorectal carcinoma HCT 116 cells. Cell permeable.
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cIAP1 and cIAP2 facilitate cancer cell survival by functioning as E3 ligases that promote RIP1 ubiquitination.
Bertrand et al.
Mol. Cell, 2008;30:689
Smac mimetics and innate immune stimuli synergize to promote tumor death.
Beug et al.
Cytoprotective effects of IAPs revealed by a small molecule antagonist.
Galbán et al.