Description
MS049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC 50 s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and does not affect the growth of HEK293 cellsIn VitroMS049 (0.1-10 µM; 20 hours) reduces the H3R2me2a mark in HEK293 cells in a concentration dependent manner (IC 50 =0.97±0.05 µM). MS049 (0.1-100 µM; 72 hours) inhibits endogenous PRMT4 methyltransferase activity in a concentration dependent manner resulting in reduced levels of cellular asymmetric arginine dimethylation of Med12 (Med12-Rme2a, IC 50 =1.4±0.1 µM) in HEK293 cells. MS049 is selective for PRMT4 and PRMT6 over a broad range of epigenetic modifiers, including other PRMTs, PKMTs, DNMTs, KDMs, and methyllysine/methylarginine reader proteins, and non-epigenetic targets. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: HEK293 cells Concentration: 0.1, 1, 10 µM Incubation Time: 20 hours Result: Reduced the H3R2me2a mark in HEK293 cells in a concentration dependent manner (IC 50 =0.97±0.05 µM). Western Blot AnalysisCell Line: HEK293 cells Concentration: 0.1, 1, 10, 100 µM Incubation Time: 72 hours Result: Reduced levels of cellular asymmetric arginine dimethylation of Med12 (Med12-Rme2a, IC 50 =1.4±0.1 µM) in HEK293 cells.IC50& Target:PRMT4 34 nM () PRMT6 43 nM () PRMT8 1600 nM ()