包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
Canonical SMILES | O=C(OCC1=CC=C(CNCCCCN(O)C(/C=C/C(OC)=O)=O)C=C1)NC2=CC=CC3=C2C=CC=C3.O |
分子式 | C28H31N3O6•H2O |
分子量 | 523.6 |
溶解度 | DMF: 25,DMSO: 25 mg/ml,DMSO:PBS (pH 7.2) (1:40): 0.02 mg/ml |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | Methylstat is a methyl ester prodrug of a Jumonji C domain-containing histone demethylase (JMJD) inhibitor that has favorable cell permeability. The free acid of methylstat inhibits JMJD2A, JMJD2C, JMJD2E, PHF8, and JMJD3 with IC50 values of approximately 4.3, 3.4, 5.9, 10, and 43 µM, respectively, in an in vitro assay. Methylstat inhibits growth of the JMJD2C-sensitive esophageal cancer cell line KYSE150 with a GI50 of 5.1 µM, whereas the free acid of methylstat did not inhibit cell growth up to 100 µM. Methylstat induces histone hypermethylation at multiple sites in a concentration-dependent manner (EC50 for H3K4me3 and H3K9me3 = 10.3 and 8.6 µM in KYSE150 cells and 6.7 ad 6.3 µM in MCF-7 cells, respectively). |