CST, 66244S, GSK343

Product Usage Information
GSK343 is supplied as a lyophilized powder. For a 5 mM stock, reconstitute the 1 mg in 369.21 μl DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used at 5 nM-5 μM for 2-48 hr.
Storage
Store lyophilized or in solution at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
Background
GSK343 inhibits EZH2 and EZH1 histone-lysine N-methyltransferase activity through competitive inhibition of the cofactor S-Adenosyl-l-methionine (SAM). IC values for EZH2 and EZH1 are 4 nM and 60 nM, respectively (1). Research studies show that GSK343 displays more than 1000-fold selectivity relative to other methyltransferases (1,2). These studies demonstrate that GSK343 induces cancer cell autophagy and enhances the anti-cancer effects of the multi-kinase inhibitor, sorafenib (3).
Alternate Names
ezh1; ezh2; h3k27; inhibitor; methylation; methyltransferase; sam cofactor