GSK126

Background: A potent, highly selective, S-adenosyl-methionine(SAM)-competitive, small-molecule inhibitor of EZH2 methyltransferase activity. GSK126 is highly selective against other methyltransferases and multiple other protein classes, even 150-fold more selective for the closest EZH1 (Kiapp = 89 nM) and more than 1,000-fold selective for 20 other human methyltransferases, including both SET-domain-containing and non-SET domain-containing methyltransferases. It decreases global H3K27me3 levels and reactivates silenced polycomb repressive complex 2 (PRC2) target genes.

Small volumes of GSK126 biochemical vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

MBS842897 is a biochemical targeting GSK126.