GSK 343

Cat. No. 6128new

GSK 343 C31H39N7O2 [1346704-33-3]

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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

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
Solubility:
Soluble to 20 mM in DMSO with gentle warming
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
1346704-33-3

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

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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Keywords: GSK 343, supplier, GSK343, potent, and, selective, EZH2, inhibitors, inhibits, lysine, methyltransferase, Tocris Bioscience, Lysine Methyltransferase Inhibitor products

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