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 ActivityGSK 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.
External Portal InformationChemicalprobes.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.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Complete Your Research
A chemical biology toolbox to study protein methyltransferases and epigenetic signaling.
Scheer et al.
Identification of potent, selective, cell-active inhibitors of the histone lysine methyltransferase EZH2.
Verma et al.
ACS Med.Chem.Lett., 2012;3:1091
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