MS023-dihydrochloride - Type I PRMT 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMS023 dihydrochlorideCat. No.: HY-19615BCAS No.: 1992047-64-9分式: CHClNO分量: 360.32作靶點(diǎn): Histone Methyltransferase作通路: Epigenetics儲存式: 4C, stored under argon* In solvent : -80C, 6 months; -20C, 1 month (stored underargon)溶解性數(shù)據(jù)體外實(shí)驗(yàn)

2、DMSO : 150 mg/mL (416.30 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.7753 mL 13.8766 mL 27.7531 mL5 mM 0.5551 mL 2.7753 mL 5.5506 mL10 mM 0.2775 mL 1.3877 mL 2.7753 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 MS023 dihydroc

3、hloride種有效選擇性的，具有細(xì)胞活性的 I 型蛋精氨酸甲轉(zhuǎn)移酶 (PRMTs) 抑制劑，對 PRMT1，PRMT3，PRMT4，PRMT6 和 PRMT8 的 IC50 分別為 30，119，83，4 和 5 nM 1。IC50 & Target IC50: 30 nM (PRMT1), 119 nM (PRMT3), 83 nM (PRMT4), 4 nM (PRMT6), 5 nM (PRMT8) 1體外研究MS023 (1-1000 nM; 48 hours) inhibits PRMT1 methyltransferase activity in MCF7 cells 1.MS0

4、23(1-1000 nM; 20 hours) inhibits PRMT6 methyltransferase activity in HEK293 cells 1.1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEWestern Blot Analysis 1Cell Line: MCF7 and HEK293 cellsConcentration: 1.4, 4, 12, 37, 111, 333, and 1000 nMIncubation Time: 48 hours for MCF7 cells; 20 hours for HEK29

5、3 cellsResult: Treatment potently and concentration-dependently reduced cellular levels of H4R3me2a(IC50=90.2 nM).Treatment concentration-dependently reduced the H3R2me2a mark (IC50=567 nM).REFERENCES1. Eram MS, et al. A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases. ACS Chem Biol.2016 Mar 18;11(3):772-81.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-3792;