GSK 343

Key Product Details

Product Description

GSK 343 is a potent and selective SAM-competitive EZH2 inhibitor (IC₅₀ = 4 nM), that exhibits >60 fold selectivity for EZH2 over EZH1 and a range of other methyltransferases. GSK 343 decreases H3K27me3 levels in breast cancer cells and inhibits proliferation of prostate cancer cell lines in vitro.

Licensing Information

This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the GSK343 probe summary on the SGC website.

External Portal Information

Chemicalprobes.org

is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of GSK 343 is reviewed on the chemical probes website.

Product Specifications for GSK 343

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for GSK 343

The following data is based on the product molecular weight 541.69.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

2 1 Recalculate

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.2 mM	9.23 mL	46.15 mL	92.30 mL
1 mM	1.85 mL	9.23 mL	18.46 mL
2 mM	0.92 mL	4.62 mL	9.23 mL
10 mM	0.18 mL	0.92 mL	1.85 mL

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 7 publications citing the usage of this product.

• Scheer A chemical biology toolbox to study protein methyltransferases and epigenetic signaling. Nat.Commun. 2019 PMID: 30604761
• Verma Identification of potent, selective, cell-active inhibitors of the histone lysine methyltransferase EZH2. ACS Med.Chem.Lett. 2012 PMID: 24900432

Product Documents for GSK 343