SM-164

Cell-permeable Smac (DIABLO) mimetic that inhibits caspase blockers XIAP, cIAP1, and cIAP2 (Ki = 36, <1, and <1.9 nM), thus inducing apoptosis [1-3]. SM-164 sensitizes cancer cells to DNA damaging agents [4]. It also prevents binding of Hsp70 to XIAP [5]. At high concentrations, it causes lytic cell death that is not apoptosis or necroptosis [6].

References:

1) H Sun et al. J. Am. Chem. Soc. 2007 129:15279

2) H Sun et al. J. Med. Chem. 2010 53:6361

3) J Lu et al. Cancer Res. 2008 68:9384

4) J Chen et al. Mol. Med. Rep. 2019 19:5079

5) LC Cesa et al. J. Biol. Chem. 2018 293:2370

6) MA Miles et al. Apoptosis 2020 25:500