Very high affinity and selective EZH2 inhibitor
GSK 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. Promotes the transition of ESCs to feeder-free extended pluripotent stem (EPS) cells in combination with LCDM cocktail .
| Marque | Tocris |
|---|---|
| Réf. B-LABO | BL-RE-124607 |
| Réf. fabricant | 18787606 |
| Nom chimique ou matériau | <i>N</i>-[(1,2-Dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-3-methyl-1-[(1<i>S</i>)-1-methylpropyl]-6-[6-(1-piperazinyl)-3-pyridinyl]-1<i>H</i>-indole-4-carboxamide |
| CAS | 1346574-57-9 |
| Quantité | 5 mg |
| Formule moléculaire | C<sub>31</sub>H<sub>38</sub>N<sub>6</sub>O<sub>2</sub> |
| Poids de la formule | 526.67 |
| Type de produit | Inhibitor |
| Pureté | 98% |
