A selective

GSK343 – 5 mg

Brand:
Cayman
CAS:
1346704-33-3
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} GSK343 is a cell-permeable EZH2 inhibitor (IC50 = 4 nM) that is 60-fold selective over EZH1 and >1,000-fold selective over other histone methytranferases.{24979} GSK343 has been shown to inhibit the trimethylation of H3K27 in HCC1806 cells with an IC50 value of 174 nM.{24979} See Structural Genomics Consortium (SGC) website for more information.  

 

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Description

A selective, cell-permeable EZH2 inhibitor (IC50 = 4 nM) that has been shown to inhibit the trimethylation of H3K27 in HCC1806 cells with an IC50 value of 174 nM

Formal name: N-[(1,2-dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[2-(4-methyl-1-piperazinyl)-4-pyridinyl]-1H-indazole-4-carboxamide

Synonyms: 

Molecular weight: 541.7

CAS: 1346704-33-3

Purity: ≥95%

Formulation: A crystalline solid

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

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