Purpose: To explore the effects and mechanisms of GSK126, a novel inhibitor of histone methyltransferase enhancer of zeste homologue 2, on cancer cell migration. Methods: Gastric …

Jul 22, 2022 · GSK126, a highly selective inhibitor of EZH2 methyltransferase activity influenced H3K27me3 chromatin content and transcriptional control resulting in the expression of core β …

Jul 28, 2020 · GSK126 (GSK2816126) can inhibit wild type and Y641 mutant EZH2 with similar potency and is highly selective compared to EZH1 (150-fold increased potency) or 20 other …

Oct 10, 2012 · Here we demonstrate that GSK126, a potent, highly selective, S -adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase activity, …

GSK126 (GSK2816126A) is a potent, highly selective inhibitor of EZH2 methyltransferase with an IC50 of 9.9 nM. - Mechanism of Action & Protocol.

Dec 6, 2012 · Here we demonstrate that GSK126, a potent, highly selective, S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase activity, …

Jan 10, 2017 · GSK126 treatment elicited caspase-3-dependent MCL-1 cleavage with accumulation of proapoptotic truncated MCL-1. These results suggested that GSK126 triggers …

We investigated the effect of EZH2 inhibition on MM cells using a potent inhibitor (GSK126). The results showed that GSK126 effectively abrogated the methylated histone 3 (H3K27me3) level …

Feb 22, 2016 · In the present study, we have demonstrated that suppressing EZH2 expression by GSK126 significantly inhibits cell migration, angiogenesis and tumor metastasis. Thus, our …

Inhibits EZH2 mutant tumor growth in xenograft models. Reactivates silenced PRC2 target genes and inhibits the proliferation of EZH2 mutant DLBCL cell lines and corresponding xenografts …