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$0.00 - Nie L, .et al. CDK2-mediated site-specific phosphorylation of EZH2 drives and maintains triple-negative breast cancer, Nat Commun, 2019, Nov 8;10(1):5114 PMID: 31704972
- Yang PM, .et al. p38α/S1P/SREBP2 activation by the SAM-competitive EZH2 inhibitor GSK343 limits its anticancer activity but creates a druggable vulnerability in hepatocellular carcinoma, Am J Cancer Res, 2019, Oct 1;9(10):2120-2139 PMID: 31720078
Biological Activity
GSK343 is a potent histone H3-lysine 27 (H3K27) methyltransferase EZH2 inhibitor (IC= 4 nM). Diplays 1000-fold selectivity for other HMTs except EZH1 (60-fold selectivity). GSK343 inhibits H3K27 methylation in HCC1806 cells with an IC of <200nM (measured by immunofluorescence).
Targets
| EZH2 (Cell-free assay) | EZH1 (Cell-free assay) | |||
| 4 nM | 240 nM |
| In vitro | DMSO | 1 mg/mL heating (1.84 mM) | |
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | 4 mg/mL (7.38 mM) | ||
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 18.46 mL | 92.3 mL | 184.61 mL |
| 0.5 mM | 3.69 mL | 18.46 mL | 36.92 mL |
| 1 mM | 1.85 mL | 9.23 mL | 18.46 mL |
| 5 mM | 0.37 mL | 1.85 mL | 3.69 mL |
*The above data is based on the productmolecular weight 541.69. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A13114 |
|---|---|
| Actions | Inhibitor |
| M. Wt | 541.69 |
| Formula | C31H39N7O2 |
| Solubility | DMSO |
| Purity | >98% |
| Storage | at -20°C 3 years Powder |
| CAS No. | 1346704-33-3 |
| Synonyms | GSK-343, GSK 343 |
| SMILES | CCCC1=C(C(=O)NC(=C1)C)CNC(=O)C2=C3C=NN(C3=CC(=C2)C4=CC(=NC=C4)N5CCN(CC5)C)C(C)C |
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