S89439 |
DC-S239 |
源叶(MedMol) | 98% |
- 产品描述: DC-S239 is a selective histone methyltransferase SET7 inhibitor with an IC50 value of 4.59 μM. DC-S239 also displays selectivity for DNMT1, DOT1L, EZH2, NSD1, SETD8 and G9a. DC-S239 has anticancer activity
- 靶点: IC50: 4.59 μM (SET7);HistoneMethyltransferase
- 体外研究:
DC-S239 inhibits DNMT1, DOT1L, EZH2, NSD1, SETD8 and G9a by less than 45%, while it inhibits SET7 by 90% at concentrations of 100 μM. DC-S239 (0-100 μM, 120 h) can inhibit the proliferation of MCF7, HL60 and MV4-11 cells in a dose-dependent manner but no significant effect on the activity of HCT116 and DHL4 cells. Cell Viability Assay Cell Line: MCF7, HL60, DHL4, MV4-11 and HCT116 cell lines Concentration: 0-100 μM Incubation Time: 120 h Result: Inhibited MCF7 and HL60 with the IC50 values of 10.93 μM and 16.43 μM, respectively.
- 参考文献:
1. Fanwang Meng, et al. Discovery and Optimization of Novel, Selective Histone Methyltransferase SET7 Inhibitors by Pharmacophore- and Docking-Based Virtual Screening. J Med Chem. 2015 Oct 22;58(20):8166-81.
- 溶解性: Soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.862 ml 14.312 ml 28.624 ml 5 mM 0.572 ml 2.862 ml 5.725 ml 10 mM 0.286 ml 1.431 ml 2.862 ml 50 mM 0.057 ml 0.286 ml 0.572 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)