GNE-375

GNE-375 is a potent, selective BRD9 inhibitor with IC50 of 5 nM, displays >480-fold selectivity over BRD4, CECR2, and TAF1; decreases BRD9 binding to chromatin, and decreases expression of ALDH1A1, a gene previously shown to be important in drug tolerance; shows remarkable potency in preventing the emergence of a drug tolerant population in EGFR mutant PC9 cells treated with EGFR inhibitors.

References 1. Crawford TD, et al. Bioorg Med Chem Lett. 2017 Aug 1;27(15):3534-3541. View Related Products by Target Bromodomain