1. Epigenetics
  2. Histone Methyltransferase
  3. 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.

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DC-S239

DC-S239 Estructura química

No. CAS : 303141-21-1

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10 mM * 1 mL in DMSO
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Descripciòn

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].

IC50 & Target

DOT1L

 

EHMT2/G9a/KMT1C

 

Cellular Effect
Cell Line Type Value Description References
HL-60 IC50
16.43 μM
Compound: DC-S239
Cytotoxicity against human HL60 cells assessed as inhibition of cell proliferation after 120 hrs by alamar blue assay
Cytotoxicity against human HL60 cells assessed as inhibition of cell proliferation after 120 hrs by alamar blue assay
[PMID: 26390175]
MCF7 IC50
10.93 μM
Compound: DC-S239
Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation after 120 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation after 120 hrs by MTT assay
[PMID: 26390175]
In Vitro

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Peso molecular

349.36

Fòrmula

C15H15N3O5S

No. CAS
Appearance

Solid

Color

Yellow to orange

SMILES

O=C(OCC)C1=C(SC(C(NC2=CC=CC([N+]([O-])=O)=C2)=O)=C1C)N

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvente y solubilidad
In Vitro: 

DMSO : 125 mg/mL (357.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8624 mL 14.3119 mL 28.6238 mL
5 mM 0.5725 mL 2.8624 mL 5.7248 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8624 mL 14.3119 mL 28.6238 mL 71.5594 mL
5 mM 0.5725 mL 2.8624 mL 5.7248 mL 14.3119 mL
10 mM 0.2862 mL 1.4312 mL 2.8624 mL 7.1559 mL
15 mM 0.1908 mL 0.9541 mL 1.9083 mL 4.7706 mL
20 mM 0.1431 mL 0.7156 mL 1.4312 mL 3.5780 mL
25 mM 0.1145 mL 0.5725 mL 1.1450 mL 2.8624 mL
30 mM 0.0954 mL 0.4771 mL 0.9541 mL 2.3853 mL
40 mM 0.0716 mL 0.3578 mL 0.7156 mL 1.7890 mL
50 mM 0.0572 mL 0.2862 mL 0.5725 mL 1.4312 mL
60 mM 0.0477 mL 0.2385 mL 0.4771 mL 1.1927 mL
80 mM 0.0358 mL 0.1789 mL 0.3578 mL 0.8945 mL
100 mM 0.0286 mL 0.1431 mL 0.2862 mL 0.7156 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

Nombre del producto:
DC-S239
Cat. No.:
HY-121093
Cantidad:
MCE Japan Authorized Agent: