GSK126, EZH2 methyltransferase inhibitor (ab269816)
Key features and details
- Potent and selective EZH2 methyltransferase inhibitor
- CAS Number: 1346574-57-9
- Soluble in DMSO to 5 mM
- Form / State: Solid
- Source: Synthetic
製品の概要
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製品名
GSK126, EZH2 methyltransferase inhibitor -
製品の詳細
Potent and selective EZH2 methyltransferase inhibitor -
生理活性の詳細
Potent inhibitor EZH2 methyltransferase inhibitor (Ki = 93 pM). Selective (>150-fold) versus EZH1. Greater than 1000-fold selective against a panel of 20 other human methyltransferases including both SET-domain-containing and non-SET-domain-containing methyltransferases. Decreases global H3K27me3 levels. Inhibits B-cell lymphoma cell proliferation in vitro. Inhibits EZH2 mutant tumor growth in xenograft models. Reactivates silenced PRC2 target genes and inhibits the proliferation of EZH2 mutant DLBCL cell lines and corresponding xenografts mice. Literature suggests that GSK126 is a potential treatment for EZH2 mutant lymphoma (McCabe et al)
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CAS 番号
1346574-57-9 -
構造式
製品の特性
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体系名
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 -
分子量
526.67 -
分子式
C31H38N6O2 -
PubChem 登録番号
68210102 -
保存方法
Shipped at room temperature. Store at -20°C. -
溶解性
Soluble in DMSO to 5 mM -
使用に関する注意
Refer to SDS for further information.
Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
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SMILES 線形表記
CC[C@H](C)N1C=C(C2=C(C=C(C=C21)C3=CN=C(C=C3)N4CCNCC4)C(=O)NCC5=C(C=C(NC5=O)C)C)C -
由来
Synthetic
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研究分野
画像
プロトコール
To our knowledge, customised protocols are not required for this product. Please try the standard protocols listed below and let us know how you get on.
参考文献 (0)
ab269816 は論文での使用が確認できていません。