GSK126 | EZH2 methyltransferase inhibitor
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $70.00 | ||
| 25 mg | $325.00 |
GSK126 (1346574-57-9) is a 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
References/Citations:
- McCabe et al. (2012), EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations; Nature 492 108
- Barili et al. (2020), Targeting p53 and histone methyltransferases restores exhausted CD8+ T cells in HCV infection; Nat. Commun. 11 604
- Zheng et al. (2021), Derivation of feeder-free human extended pluripotent stem cells; Stem Cell Rep. 16 1686
- Wang et al. (2022), GSK-126 Protects CA1 Neurons from H3K27me3-mediated Apoptosis in Cerebral Ischemia; Mol. Neurobiol. 59 2552
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
GSK126 (1346574-57-9) is a 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
References/Citations:
- McCabe et al. (2012), EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations; Nature 492 108
- Barili et al. (2020), Targeting p53 and histone methyltransferases restores exhausted CD8+ T cells in HCV infection; Nat. Commun. 11 604
- Zheng et al. (2021), Derivation of feeder-free human extended pluripotent stem cells; Stem Cell Rep. 16 1686
- Wang et al. (2022), GSK-126 Protects CA1 Neurons from H3K27me3-mediated Apoptosis in Cerebral Ischemia; Mol. Neurobiol. 59 2552
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