GSK-126
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- 应用范围
- Inhibition (Inh)
- 原理
- EZH2 Histone methyltransferase inhibitor
- 产品特性
- 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.
- 纯度
- >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).
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- 限制
- 仅限研究用
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- 状态
- Powder
- 储存条件
- -20 °C
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- 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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