Chemical structure of GSK343.
Western blot analysis of extracts from HeLa cells, untreated (-) or treated with GSK343 (48 hr) at the indicated concentrations, using Tri-Methyl-Histone H3 (Lys27) (C36B11) Rabbit mAb #9733 (upper) and Histone H3 (D1H2) XP® Rabbit mAb #4499 (lower).
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.
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.
GSK343 inhibits EZH2 and EZH1 histone-lysine N-methyltransferase activity through competitive inhibition of the cofactor S-Adenosyl-l-methionine (SAM). IC50 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).
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