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- 产品描述: 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.
- 靶点: Histone Methyltransferase;HistoneMethyltransferase
- 体外研究:
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.
- 细胞实验: 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.
- 参考文献:
1. Shen Y,etal.Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6.J Med Chem. 2016 Oct 13;59(19):9124-9139.
- 溶解性: soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 4.026 ml 20.132 ml 40.264 ml 5 mM 0.805 ml 4.026 ml 8.053 ml 10 mM 0.403 ml 2.013 ml 4.026 ml 50 mM 0.081 ml 0.403 ml 0.805 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)