GSK126GSK126 is a potent, highly selective, S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase with Ki value of 0.5 nM.
IC50 Value: 0.5 nM (Ki)
Target: EZH2
in vitro: Although GSK126 induced loss of H3K27me3 independent of EZH2 mutation status, six of seven lymphoma cell lines sensitive to GSK126 treatment were EZH2-mutation(+), while only two of 11 lymphoma cell lines less sensitive to GSK126 were EZH2-mutation(+) [1].
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Description: GSK2606414 GSK2606414 is an orally available, potent, and selective PERK inhibitor with an IC50 of 0.4 nM. IC50 Value: 0.4 nM [1] Target:PERK GSK2606414 inhibits PERK activation in cells and inhibits the growth of a human tumor xenograft in mice. Tar...