For research use only. Not for therapeutic Use.
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].
| Catalog Number | I025621 |
| CAS Number | 303141-21-1 |
| Synonyms | ethyl 2-amino-4-methyl-5-[(3-nitrophenyl)carbamoyl]thiophene-3-carboxylate |
| Molecular Formula | C15H15N3O5S |
| Purity | ≥95% |
| InChI | InChI=1S/C15H15N3O5S/c1-3-23-15(20)11-8(2)12(24-13(11)16)14(19)17-9-5-4-6-10(7-9)18(21)22/h4-7H,3,16H2,1-2H3,(H,17,19) |
| InChIKey | SIVTXLSKYVOFHS-UHFFFAOYSA-N |
| SMILES | CCOC(=O)C1=C(SC(=C1C)C(=O)NC2=CC(=CC=C2)[N+](=O)[O-])N |
| Reference | [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. |
