SKU: C-1158-5mg
GSK-126 Chemical Formula: C31H38N6O2 Solid Powder
  • Catalog#: C-1158
  • Targets: EZH2
  • Synonym: GSK2816126; GSK-2816126; GSK 2816126; GSK-126; GSK126; GSK-126
  • Chemical Name/IUPAC:(S)-1-(sec-butyl)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide
    Technical Data
  • Product Name: GSK-126
  • Chemical Formula: C31H38N6O2
  • Molecular Weight: 526.67
  • CAS#: 1346574-57-9
  • Appearance: Solid powder
  • Purity: > 99% by HPLC
  • Solubility: Soluble in DMSO
  • Storage: Room temperature for months, or -20ºC for 3 years
    GSK-126 is a potent, highly selective, S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase activity. GSK-126 decreases global H3K27me3 levels and reactivates silenced PRC2 target genes. GSK-126 effectively inhibits the proliferation of EZH2 mutant DLBCL cell lines and markedly inhibits the growth of EZH2 mutant DLBCL xenografts in mice. Together, these data demonstrate that pharmacological inhibition of EZH2 activity may provide a promising treatment for EZH2 mutant lymphoma.