Description
EPZ020411 is a potent, selective PRMT6 inhibitor with IC50 of 10nM, 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 0.637uM, 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