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. Alternate Names: GSK-2816126
EZH2 methyltransferase inhibitor
Molecular Weight:
526.69
Purity:
98% by HPLC/TLC, NMR (Conforms)
Form:
Cream colored solid
CAS Number:
[1346574-57-9]
Formula:
C31H38N6O2
Application Notes:
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
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