MS 049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC 50 of 34 nM and 43 nM respectively.target: PRMT4, PRMT6;IC 50: 34 nM (PRMT4 ), 43 nM (PRMT6 );In vitro: MS 049 reduces the H3R2me2a mark in HEK293 cells in a concentration dependent manner. MS 049 treatment (72 h exposure) inhibits endogenous PRMT4 methyltransferase activity in a concentration dependent manner resulting in reduced levels of cellular asymmetric arginine dimethylation of Med12 (Med12-Rme2a, IC50 = 1.4 ± 0.1 μM (n = 3)) in HEK293 cells.
[1]. Shen Y et al. Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6. J Med Chem. 2016 Sep 15.