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.

PRMT6:43 nM, PRMT4:34 nM

在细胞实验中，MS049 强效抑制 PRMT4 和 PRMT6 的甲基转移酶活性，并降低 HEK293 细胞中 Med12me2a 和 H3R2me2a 的水平。在 50 μM 浓度下，MS049 对任何甲基转移酶都不表现出抑制作用，在 10 μM 下也不抑制任何去甲基化酶，且在 200 μM 的 DSF 实验中，对任何甲基赖氨酸/甲基精氨酸阅读蛋白均不显示出明显的结合。

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.