A-1210477 is a potent and selective MCL-1 and Bcl-2 inhibitor with Ki and IC50 of 0.454 nM and 26.2 nM, respectively, >100-fold selectivity over other Bcl-2 family members.

99%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

10 mM in DMSO

MCL-1

In H929 cells, A-1210477 binds to MCL-1 with high affinity and induces MCL-1 protein elevation. In H929, H2110, and H23 cells, A-1210477 induce the hallmarks of apoptosis, and inhibits MCL-1-dependent cell viability. A-1210477 also synergizes with navitoclax to kill a variety of cancer cell lines. In SKBR3 cells, A-1210477 inhibits MCL-1–BIM interaction and induces classical features of apoptosis. In addition, A-1210477 sensitizes non-Hodgkin’s lymphoma cell lines to venetoclax (ABT-199).

1. Bruncko M, et al. J Med Chem. 2015 Mar 12;58(5):2180-2194.

2. Leverson JD, et al. Cell Death Dis. 2015 Jan 15;6:e1590.