GSK343

Catalog No.: A13114

EZH2 inhibitor

GSK343

GSK343 Chemical Structure

CAS NO. 1346704-33-3

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).

Availability: In stock

Package Price Qty
5 mg
$50.00
10 mg
$80.00
25 mg
$150.00
50 mg
$250.00
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Warning Products are for laboratory research use only. Not for human use. We do not sell to patients.
  • 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 nM240 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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