Potent and selective SAM-competitive EZH2 inhibitor (IC50 = 4 mM). Exhibits >60 fold selectivity for EZH2 over EZH1 and a range of other methyltransferases. Inhibits proliferation of prostate cancer cell lines in vitro.
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.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|DMSO||10.83||20mM with gentle warming|
Preparing Stock Solutions
The following data is based on the product molecular 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.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.85 mL||9.23 mL||18.46 mL|
|5 mM||0.37 mL||1.85 mL||3.69 mL|
|10 mM||0.18 mL||0.92 mL||1.85 mL|
|50 mM||0.04 mL||0.18 mL||0.37 mL|
References are publications that support the products' biological activity.
Verma et al (2012) Identification of potent, selective, cell-active inhibitors of the histone lysine methyltransferase EZH2. ACS Med.Chem.Lett. 3 1091 PMID: 24900432
If you know of a relevant reference for GSK 343, please let us know.
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Literature in this Area
Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.