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
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 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.

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


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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
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.

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