GSK-126

SKU: C-1158

Made in USA, High-Purity Standard Quality

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Catalog#: C-1158

Quantity: 5mg

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

Description
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.

GSK-126

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