规格: | 98% |
分子量: | 349.36 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
Background:
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[1].
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[1].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[1].
[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.