MS049 是一种有效的、选择性的和细胞活性的 PRMT4 和 PRMT6 双重抑制剂，IC50 分别为 34 和 43 nM。它可降低 HEK293 细胞的 Med12me2a 和 H3R2me2a 水平。

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.

In cellular assays, MS049 potently inhibits the methyltransferase activity of PRMT4 and PRMT6 and reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 does not inhibit any of the methyltransferases at 50 μM or demethylases at 10 μM and does not display appreciable binding to any of the methyllysine/methylarginine reader proteins using the DSF assay at 200 μM.

HEK293 cells grown in DMEM supplemented with 10% FBS, penicillin (100 U/mL), and streptomycin (100 μg/mL) were seeded on 96-well plates at density 3000/well and treated with compounds at 0, 1, 10, and 50 μM concentrations for 96 h. The confluency was measured using IncuCyte ZOOM live cell imaging device and analyzed with IncuCyte ZOOM software based on phase contrast images.

1502816-23-0

C15H24N2O

248.37

DMSO:31 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years