MS049

MS049 是一种高效、选择性和细胞活性的 PRMT4 和 PRMT6 双重抑制剂，IC50 分别为 34 nM 和 43 nM。MS049 降低了 HEK293 细胞的 Med12me2a 和 H3R2me2a 水平。MS049 对 HEK293 细胞无毒，并且没有影响其的生长。 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 cells In Vitro MS049 (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 ()

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