Product Name: GSK-343

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CAT#: A-1416


  Synonym:GSK343

GSK-343 Chemical Structure
GSK-343 chemical structure


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IUPAC/Chemical name: 1-isopropyl-N-((6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl)-6-(2-(4-methylpiperazin-1-yl)pyridin-4-yl)-1H-indazole-4-carboxamide.

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Biological Activity

GSK-343 is a potent EZH2 inhibitor.
A potent histone H3-lysine 27 (H3K27) methyltransferase EZH2 inhibitor (IC= 4 nM). Diplays 1000-fold selectivity for other HMTs except EZH1 (60-fold selectivity). GSK343 inhibits H3K27 methylation in HCC1806 cells with an IC of <200nM (measured by immunofluorescence).

The histone H3-lysine 27 (H3K27) methyltransferase EZH2 plays a critical role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer. GlaxoSmithKline has developed a potent, selective, cell-active EZH2 inhibitor, GSK343, and has made this available as a chemical probe as part of the SGC epigenetics initiative. GSK343 inhibits EZH2 with an IC50 of 4nM and is over 1000-fold selective for other HMTs except EZH1 (60-fold selectivity). GSK343 inhibits H3K27 methylation in HCC1806 cells with an IC50 of <200nM as measured by immunofluorescence.
For full characterization details, please visit the UNC1215 probe summary on the Structural Genomics Consortium (SGC) website.

Technical Data

M.Wt: 541.69
Molecular Formula: C31H39N7O2
CAS#: 1346704-33-3
Purity: >99%
Storage Conditions: 2ºC to 8 ºC, or -20ºC for 3 years.
GSK-343 MSDS GSK-343 CoA

Reference



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