GSK-126isaninhibitorofmutantEZH2,ahistonemethyltransferase(HMT)thatexhibitspointmutationsatkeyresiduesTyr641andAla677;thiscompounddoesnotappreciablyaffectWTEZH2.EZH2isresponsIBLeformodulatingexpressionofavarietyofgenes.GSK-126competeswithcofactorS-adenylmethionine(SAM)forbindingtoEZH2.GSK-126displaysanticancerchemotherapeuticactivitybyinhibitingproliferationininvitroandinvivomodelsofdiffuselargeB-celllymphoma.
| CasNo. | 1346574-57-9 |
|---|---|
| Purity | ≥99%,≥99%ee |
| Formula | C31H38N6O2 |
| FormulaWt. | 526.67 |
| IUPACName | 1-[(2S)-butan-2-yl]-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-methyl-6-(6-piperazin-1-ylpyridin-3-yl)indole-4-carboxamide |
| Solubility | SolubleinDMSO |
| Appearance | tanpowder |
| StoreTemp | -20°C |
|---|---|
| ShipTemp | Ambient |
| MSDS | G7340MSDSPDF |
|---|---|
| InfoSheet | G7340InfoSheetPDF |
| Brochures | EpigeneticModifiersBooklet |
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McCabeMT,OttHM,GanjiG,etal.EZH2inhibitionasatherapeuticstrategyforlymphomawithEZH2-activatingmutations.Nature.2012Dec6;492(7427):108-12.PMID:23051747.
