Application

GSK343 has been used:as an inhibitor ofenhancer of zeste homolog 2 (EZH2) to assess the impact of chromatin condensation oncell migrationas histone methyl transferase inhibitor, to suppress the Polyandrocarpa misakiensis, mitochondrial non-coding-region (NCR) PmNCRreporter gene expression, facilitatedby TC14-3as a supplement in the growth medium to inhibit the generation of H3K27me3 or to inhibit RNA polymerase IIas EZH2 inhibitor to treat castration-resistant neuroendocrine prostate cancer (CRPC-NE)

Biochem/physiol Actions

GSK343 is a potent, specific inhibitor of the histone H3-lysine 27 (H3K27) methyltransferase EZH2. GSK343 inhibits EZH2 enzymatic activity with an IC₅₀ of 4 nM. The compound displays 60 fold selectivity for EZH2 vs. EZH1, and 1000 fold or greater selectivity against other histone methyltransferases. The IC₅₀ for inhibition of H3K27 methylation is ﹤ 200 nM in HCC1806 cells. For full characterization details, please visit the GSK343 probe summary on the Structural Genomics Consortium (SGC) website.To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc

Features and Benefits

GSK343 is an epigenetic chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC epigenetic probes, visit sigma.com/SGC.

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Other Notes

GSK343 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the GSK343 probe summary on the Chemical Probes Portal website.

Packaging

5, 25 mg in glass bottle