GSK126
EZH2 methyltransferase inhibitor / Potent, selective, S-adenosyl-methionine-competitive inhibitor of EZH2 methyltransferase, Ki=0.5-3 nM, >150-fold selective for EZH2 over EZH1 and >1000-fold selective over 20 methyltransferases.1 Decreases global H3K27me3 levels and reactivates silenced PRC2 target genes. GSK-126 inhibits proliferation of diffuse large B-cell lymphoma (DLBCL) cell lines as well as DLBCL xenografts in mice.1 Rescues exhausted CD8+ T cells in HCV infection.2 Facilitates the transition of embryonic stem cells to feeder-free extended pluripotent stem cells in combination with a cocktail of other agents.3 Displays neuroprotective effects in ischemic brain injury in a rodent model.4
Biochemicals & reagents
1346574-57-9
GSK-2816126
1 McCabe et al. (2012), EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations; Nature 492 108 2 Barili et al. (2020), Targeting p53 and histone methyltransferases restores exhausted CD8+ T cells in HCV infection; Nat. Commun. 11 604 3 Zheng et al. (2021), Derivation of feeder-free human extended pluripotent stem cells; Stem Cell Rep. 16 1686 4 Wang et al. (2022), GSK-126 Protects CA1 Neurons from H3K27me3-mediated Apoptosis in Cerebral Ischemia; Mol. Neurobiol. 59 2552
-20°C
TARGET: Protein methyltransferase -- PATHWAY: Chromatin; Posttranslational modification; Transcription; Cell migration -- RESEARCH AREA: Epigenetics; Cancer stem cells; Ubiquitin/Proteasome; Stem cells -- DISEASE AREA: Cancer; InflammationPain; Neurodegeneration