DATASHEET
Formulation
Yellow solid
Storage:
-20°C
Product Information:
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
Description:
CAS Number: 1346574-57-9<br></br>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<br></br>Molecular weight: 526.69<br></br>Formula: C31H38N6O2<br></br>Solubility: DMSO (16 mg/ml)<br></br>Physical Properties: Cream colored solid<br></br>Purity: 98% by HPLC/TLC, NMR (Conforms)