Chemical Name: N-[(1,2-Dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-3-methyl-1-[(1S)-1-methylpropyl]-6-[6-(1-piperazinyl)-3-pyridinyl]-1H-indole-4-carboxamide
Biological ActivityGSK 126 is a very high affinity and selective EZH2 inhibitor (Ki = 0.5 - 3 nM). Exhibits >150-fold selectivity for EZH2 over EZH1 and >1000-fold selectivity over 20 other human methyltransferases. Inhibits proliferation of B-cell lymphoma cell lines in vitro. Also inhibits H3K27Me3 and tumor growth in mice bearing BCL xenografts. Targeting p53 and histone methyltransferases restores exhausted CD8+ T cells in HCV infection.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations.
McCabe et al.
Targeting p53 and histone methyltransferases restores exhausted CD8+ T cells in HCV infection.
Barili et al.
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