MS049 dihydrochloride 是一种有效的、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 dihydrochloride 降低了 HEK293 细胞的 Med12me2a 和 H3R2me2a 水平。MS049 dihydrochloride 无毒,不影响 HEK293 细胞的生长。
产品描述
MS049 dihydrochloride 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 dihydrochloride reduces Med12me2a and H3R2me2a levels in HEK293 cells. MS049 dihydrochloride is not toxic and does not affect the growth of HEK293 cells [1].
体外活性
MS049 dihydrochloride (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) [1]. MS049 dihydrochloride (0.1-100 μM; 72 hours) inhibits endogenous PRMT4 methyltransferase activity in a concentration dependent manner causing reduced levels of cellular asymmetric arginine dimethylation of Med12 (Med12-Rme2a, IC 50 =1.4±0.1 μM) in HEK293 cells [1]. MS049 dihydrochloride 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 [1]. Western Blot Analysis [1] Cell 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 Analysis [1] Cell 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.
Cas No.
2095432-59-8
分子式
C15H26Cl2N2O
分子量
321.29
别名
MS049 dihydrochloride
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years