as an inhibitor of?enhancer of zeste homolog 2 (EZH2) to assess the impact of chromatin condensation on?cell migration
as histone methyl transferase inhibitor, to suppress the Polyandrocarpa misakiensis, mitochondrial non-coding-region (NCR) PmNCR?reporter gene expression, facilitated?by TC14-3
as a supplement in the growth medium to inhibit the generation of H3K27me3 or to inhibit RNA polymerase II
as 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
