Dc-s239

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].

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Histone Methyltransferase

IC50: 4.59 μM (SET7)[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]. Cell Viability Assay[1] 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.

[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.