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GSK126

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
产品编号 ABIN7233255
发货至: 中国
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Quick Overview for GSK126 (ABIN7233255)

应用范围

Inhibition (Inh)

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
  • 原理

    EZH2 Histone methyltransferase inhibitor

    产品特性

    A potent, selective, S-adenosyl-methionine-competitive inhibitor of EZH2 methyltransferase, Ki=0.5-3 nM, >150-fold selective for EZH2 over EZH1 and >1000-fold selective over 20 methyltransferases1. Decreases global H3K27me3 levels and reactivates silenced PRC2 target genes. GSK126 inhibits proliferation of diffuse large B-cell lymphoma (DLBCL) cell lines as well as DLBCL xenografts in mice1. Rescues exhausted CD8+ T cells in HCV infection2. Facilitates the transition of embryonic stem cells to feeder-free extended pluripotent stem cells in combination with a cocktail of other agents3. Displays neuroprotective effects in ischemic brain injury in a rodent model4.

    纯度

    >98 %

    Formula

    C31H38N6O2

    Solubility

    Soluble in DMSO (up to 16 mg/ml)
  • 应用备注

    Optimal working dilution should be determined by the investigator.

    限制

    仅限研究用
  • 状态

    Powder

    储存条件

    -20 °C

    储存方法

    -20°C
  • 背景

    GSK-2816126,Cell migration,Epigenetics,Transcription,Protein methyltransferase,Stem cells,Cancer stem cells,Ubiquitin/Proteasome,Inflammation,Cancer,Neurodegeneration,Posttranslational modification,Pain,Chromatin

    分子量

    526.7

    CAS-编号

    1346574-57-9
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