GSK 343

Pricing Availability Delivery Time Qty
Cat.No. 6128 - GSK 343 | C31H39N7O2 | CAS No. 1346704-33-3
Description: Potent and selective SAM-competitive EZH2 inhibitor
Chemical Name: N-[(1,2-Dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[2-(4-methyl-1-piperazinyl)-4-pyridinyl]-1H-indazole-4-carboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

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.

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.

Technical Data

M. Wt 541.69
Formula C31H39N7O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1346704-33-3
PubChem ID 71268957
InChI Key ULNXAWLQFZMIHX-UHFFFAOYSA-N
Smiles CCCC1=C(C(NC(C)=C1)=O)CNC(C2=C3C=NN(C3=CC(C4=CC=NC(N5CCN(CC5)C)=C4)=C2)C(C)C)=O

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 10.83 20 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

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Product Datasheets

Safety Datasheet

References

References are publications that support the biological activity of the product.

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


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View all EZH2 Inhibitors

Keywords: GSK 343, GSK 343 supplier, GSK343, potent, and, selective, EZH2, inhibitors, inhibits, lysine, methyltransferase, PRC2, polycomb, repressive, complex, 2, Lysine, Methyltransferases, 6128, Tocris Bioscience

Citations for GSK 343

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Epigenetics

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.

Stem Cells

Stem Cells Scientific Review

Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.

Epigenetics

Epigenetics Research Bulletin

Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:

  • Bromodomains
  • DNA Methyltransferases
  • Histone Deacetylases
  • Histone Demethylases
  • Histone Methyltransferases
Cancer Metabolism

Cancer Metabolism Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the main targets for cancer metabolism researchers. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways. These distinct metabolic circuits could provide viable cancer therapeutic targets.

Epigenetics in Cancer

Epigenetics in Cancer Poster

Adapted from the 2015 Cancer Product Guide Edition 3, this poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.

Stem Cells

Stem Cells Poster

Written by Rebecca Quelch and Stefan Przyborski from Durham University (UK), this poster describes the isolation of pluripotent stem cells, their maintenance in culture, differentiation, and the generation and potential uses of organoids.