Description
A-1210477 is an inhibitor of the antiapoptotic Bcl-2 family protein myeloid cell leukemia-1 (Mcl-1; Ki = 0.43 nM and IC50 = 26.2 nM) that demonstrates >100-fold selectivity over other Bcl-2 family members (Kis > 0.66 μM for Bcl-2, Bcl-XL, Bcl-W, and Bfl-1). It has been shown to disrupt the interaction between Mcl-1 and pro-apoptotic BIM, inducing the hallmarks of apoptosis in Mcl-1-dependent multiple myeloma and non-small cell lung cancer cell lines.
References
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