A selective

GSK126 – 10 mg

Brand:
Cayman
CAS:
1346574-57-9
Storage:
-20
UN-No:
Non-Hazardous - /

The histone H3 lysine 27 (H3K27) methyltransferase EZH2 plays an important role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer.{18930} GSK126 is a selective, S-adenosyl-methionine-competitive small molecule inhibitor of EZH2 methyltransferase activity (Ki = 0.57 nM; IC50 = 9.9 nM versus that of EZH1: Ki = 89 nM; IC50 = 680 nM).{25456} It is more than 1,000-fold selective for EZH2 over other histone methyltranferases, including both SET-domain-containing and non-SET-domain-containing methyltransferases.{25456} At concentrations of 7-252 nM, it has been shown to inhibit global H3K27 trimethylation levels and to reactivate silenced PRC2 target genes.{25456} Furthermore, GSK126 can inhibit the proliferation of EZH2 mutant DLBCL cell lines (IC50 = 28-61 nM) as well as the growth of EZH2 mutant DLBCL xenografts in mice receiving a daily dose of 50 mg/kg.{25456}  

 

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Description

A selective, SAM-competitive small molecule inhibitor of EZH2 methyltransferase activity (Ki = 0.57 nM; IC50 = 9.9 nM versus that of EZH1: Ki = 89 nM; IC50 = 680 nM); inhibits global H3K27me3 levels, inhibiting the proliferation of EZH2 mutant DLBCL cell lines (IC50 = 28-61 nM) as well as the growth of EZH2 mutant DLBCL xenografts in mice receiving a daily dose of 50 mg/kg

Formal 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

Synonyms: 

Molecular weight: 526.7

CAS: 1346574-57-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Methyltransferases||Research Area|Epigenetics, Transcription, & Translation

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