BAY-598 - Histone Methyltransferase 抑制剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBAY-598Cat. No.: HY-19546CAS No.: 1906919-67-2分式: CHClFNO分量: 525.34作靶点: Histone Methyltransferase作通路: Epigenetics储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 125 mg/mL (237.94 mM; Need u

2、ltrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (3.96 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (3.96 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 BAY-598SMYD2 的个选择性分抑制剂。IC50 & Target SMYD2 1体外研究

3、 BAY-598 treatment blocks in vitro methylation of MAPKAPK3 by SMYD2 but has no activity against theSMYD2-related KMT SMYD3. BAY-598 treatment reduces the growth of Kras;p53 mutant PDAC cells after 9d in culture but has little impact on the growth of Kras;p53;Smyd2 mutant cells 1.PROTOCOLKinase Assay

4、 1 For SMYD2 inhibition, 10 L of BAY-598 or DMSO is first incubated with recombinant SMYD2 in methylationbuffer reaction for 1 h at 30C, and then 2 Ci of 3H-AdoMet is added to the mix and incubated overnight at30C. The reaction mixture is resolved by SDSfollowed by autoradiography, Coomassie stain,

5、or MSanalysis 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 1 Cells are seeded in 96-well plates at 2000 cells per well (optimum density for growth) in a total volume of 100L of medium containing 2% fetal bovine serum. Serially diluted BA

6、Y-598 in 100 L of medium is added tothe cells 12 h later. After 72 h of incubation, cell viability is assessed by an MTT assay according to themanufacturers instructions 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Reynoird N, et al. Coordination of stress signals by the lysine methyltransferase SMYD2 promotes pancreaticcancer. Genes Dev. 2016Apr 1;30(7):772-85.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.