GSK126
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1346574-57-9
≥98%
A crystalline solid
C31H38N6O2
526.7
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, gsk2816126
An EZH2 inhibitor; selective for EZH2 over EZH1 (IC50 = 680 nM) and a variety of SET-domain-containing and non-SET-domain-containing methyltransferases (IC50s = 13->100 µM); reduces global H3K27me3 levels in a variety of DLCBL cells expressing wild-type or mutant EZH2 at 7-252 nM; reduces tumor growth in a Pfeiffer DLBCL mouse xenograft model at 50 mg/kg per day; induces insulin production and glucose-stimulated insulin secretion in human pancreatic exocrine cells isolated from juvenile patients with type 1 diabetes or adults without diabetes at 10 µM; reduces H3K27me3 levels and induces insulin secretion and glucose-stimulated insulin secretion in primary human pancreatic ductal epithelial cells
