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GSK-126

Inh 1346574-57-9 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
Catalog No. ABIN7233255
  • Application
    Inhibition (Inh)
    Purpose
    EZH2 Histone methyltransferase inhibitor
    Characteristics
    Competitive, selective inhibitor of H3K27 methyltransferase EZH2 (Ki = 0.57 nM), over EZH1 (Ki = 89 nM) and other histone methyltransferases (Ki > 1 μM). GSK-126 caused a dose-dependent decrease in H3K27me3, and blocked invasion of triple-negative breast cancer cells. Conversely, it induced myeloid-derived suppressor cells, blocking antitumor immunity in mice. Decreases myeloma CSCs4, while also inducing differentiation of HepaRG hepatic progenitor cells5. Used to explore the role of epigenetic modification in a mouse model of Parkinson's disease.
    Purity
    >98 %
    Chemical 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
    Formula
    C31H38N6O2
    Solubility
    Soluble in DMSO (up to 15 mg/ml) or in Ethanol (up to 2 mg/ml).
  • Restrictions
    For Research Use only
  • Format
    Powder
    Storage
    -20 °C
  • Background
    GSK-2816126,Cell migration,Epigenetics,Transcription,Protein methyltransferase,Stem cells,Cancer stem cells,Ubiquitin/Proteasome,Inflammation,Cancer,Neurodegeneration,Posttranslational modification,Pain,Chromatin
    Molecular Weight
    526.7
    CAS-No
    1346574-57-9
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