产品名称 | GSK 126 |
产品货号 | Axon 2140 CAS [1346574-57-9] MF C31H38N6O2MW 526.67 Purity: 98% Optical purity: Optically pure Soluble in DMSO Description Potent, selective, cell-active inhibitor of histone lysine methyltransferase (HMTase or HMT; H3K27 selective) EZH2 (Ki 0.57 nM; IC50 9.9 nM); more than 150-fold selective for EZH2 versus EZH1 (Ki 89 nM) and 20 other human methyltransferases. GSK126 effectively inhibits proliferation of EZH2 mutant DLBCL cell lines and growth of EZH2 mutant DLBCL xenografts in mice. References Certificates Categories Extra info MT McCabe et al. EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations. Nature. 2012, 492, 108-112. SK Verma et al. Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2. ACS Med. Chem. Lett. 2012, 3, 1091−1096. Certificate of Analysis Material Safety Data Sheet Apoptosis Cell Cycle Regulation Cell Signaling & Oncology Epigenetics EC 2.1.1.43 HMTase Inhibitor of Histone Lysine Methyltransferase EZH2 Chemical name (S)-1-sec-butyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide Parent CAS No. [1346574-57-9] Order Size Unit Price Stock 2 mg €75.00 In Stock |
产品价格 | 现货询价,电话:010-67529703 |
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产品品牌 | axonmedchem |
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GSK 126Axon 2140 CAS [1346574-57-9] MF C31H38N6O2
Description
Potent, selective, cell-active inhibitor of histone lysine methyltransferase (HMTase or HMT; H3K27 selective) EZH2 (Ki 0.57 nM; IC50 9.9 nM); more than 150-fold selective for EZH2 versus EZH1 (Ki 89 nM) and 20 other human methyltransferases. GSK126 effectively inhibits proliferation of EZH2 mutant DLBCL cell lines and growth of EZH2 mutant DLBCL xenografts in mice.
Inhibitor of Histone Lysine Methyltransferase EZH2
Chemical name(S)-1-sec-butyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide Parent CAS No.[1346574-57-9] |
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