SKI-73

SKI-73 is a CARM1 chemical probe with pro-drug properties, can readily penetrate cell membranes and then be processed into two active CARM1 inhibitors.SKI-73 (10 uM) fully suppresses the methylation of BAF155 Arg1064 in MCF-7 cells.SKI-73 inhibits in vitro invasion but not proliferation of breast cancer cells ( MDA-MB-231 cell, EC50=1.3 uM).SKI-73 recapitulates the anti-invasion effect of the genetic perturbation of CARM1.Either CARM1 knockout or CARM1 inhibition with SKI-73 alters the epigenetic plasticity in a proliferation-independent manner by replacing the most invasion-prone subpopulation with the non-invasive subpopulation(s) to suppress the invasive phenotype.

1. Xiao-Chuan Cai, et al. Elife. 2019 Oct 28;8:e47110.