| Identification | Back Directory | [Name]
3-Thiophenecarboxylic acid, 2-amino-4-methyl-5-[[(3-nitrophenyl)amino]carbonyl]-, ethyl ester | [CAS]
303141-21-1 | [Synonyms]
DC-S239
3-Thiophenecarboxylic acid, 2-amino-4-methyl-5-[[(3-nitrophenyl)amino]carbonyl]-, ethyl ester | [Molecular Formula]
C15H15N3O5S | [MOL File]
303141-21-1.mol | [Molecular Weight]
349.36 |
| Chemical Properties | Back Directory | [Boiling point ]
479.4±45.0 °C(Predicted) | [density ]
1.440±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 125 mg/mL (357.80 mM; Need ultrasonic) | [form ]
Solid | [pka]
11.12±0.70(Predicted) | [color ]
Yellow to orange |
| Hazard Information | Back Directory | [Biological Activity]
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]. | [References]
[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. |
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