Fig. 1.
Effects of EPZ-6438 on cellular global histone methylation and cell viability. (A) Chemical structure of EPZ-6438. (B) Concentration-dependent inhibition of cellular H3K27Me3 levels in G401 and RD cells. (C) Selective inhibition of proliferation of SMARCB1-deleted G401 cells by EPZ-6438 in vitro (measured by ATP content). G401 and RD cells were replated at the original seeding densities on day 7. Each point represents the mean for each concentration (n = 3). (D) Proliferation IC50 values (day 14) for SMARCB1 wild-type and mutant cells. Compound incubations for each experiment were performed in triplicate, and symbols represent the mean of two experiments for all cell lines. The horizontal lines represent the median. Mean calculation of duplicate experiments was not possible for RD and SJCRH30 cells; individual values are shown (Table S2).