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.
Kinase Assay
Cell Assay
Animal Administration
References
c[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.
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