MS049

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.

Signaling Pathways >> Epigenetics >> Histone Methyltransferase

Research Areas >> Cancer

[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.

GSK126 | Tazemetostat (EPZ-6438) | UNC 0642 | GSK343 | Pinometostat (EPZ5676) | 3-Deazaneplanocin A (hydrochloride) | Pemrametostat (GSK3326595) | UNC1999 | BIX-01294 | EPZ031686 | AZ505 (ditrifluoroacetate) | MS023 | EPZ 004777 | EPZ015666 | EPZ015866(GSK591)