EPZ020411 dihydrochloride

EPZ020411 is a potent, selective PRMT6 inhibitor with IC50 of 10 nM, displays 10-fold and 20-fold selectivity over PRMT1/8, and >100-fold over other histone methyltransferases (PRMT3/4/5/7); dose-dependently decreases H3R2 methylation A375 cell line with IC50 of 0.637 uM, with no affect levels of PRMT6 expression; exhibits good bioavailability following subcutaneous dosing in rats making it a suitable tool for potential in vivo target validation studies.

References 1. Mitchell LH, et al. ACS Med Chem Lett. 2015 Apr 6;6(6):655-9. View Related Products by Target Histone Methyltransferase (HMTase)