中文名 | GSK620 |
英文名 | 1-Benzyl-N5-cyclopropyl-N3-methyl-2-oxo-1,2-dihydropyridine-3,5-dicarboxamide |
别名 | 化合物GSK620 |
英文别名 | GSK620 1-Benzyl-N5-cyclopropyl-N3-methyl-2-oxo-1,2-dihydropyridine-3,5-dicarboxamide 1-benzyl-N5-cyclopropyl-N3-methyl-2-oxo-1,2-dihydropyridine-3,5-dicarboxamide |
CAS | 2088410-46-0 |
化学式 | C18H19N3O3 |
分子量 | 325.36 |
溶解度 | 溶于DMSO |
存储条件 | -20℃ |
产品用途 | GSK620 is a Potent, selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitor. GSK620 showed an anti-inflammatory phenotype in human whole blood, confirming their cellular target engagement. Excellent broad selectivity, developability, and in vivo oral pharmacokinetics characterize these tools, which we hope will be of broad utility to the field of epigenetics research. |
参考资料 展开查看 | 1: Aylott HE, Atkinson SJ, Bamborough P, Bassil A, Chung CW, Gordon L, Grandi P, Gray JRJ, Harrison LA, Hayhow TG, Messenger C, Mitchell D, Phillipou A, Preston A, Prinjha RK, Rianjongdee F, Rioja I, Seal JT, Wall ID, Watson RJ, Woolven JM, Demont EH. Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors. J Med Chem. 2021 Mar 25;64(6):3249-3281. doi: 10.1021/acs.jmedchem.0c02156. Epub 2021 Mar 4. PMID: 33662213. 2: Seal JT, Atkinson SJ, Aylott H, Bamborough P, Chung CW, Copley RCB, Gordon L, Grandi P, Gray JRJ, Harrison LA, Hayhow TG, Lindon M, Messenger C, Michon AM, Mitchell D, Preston A, Prinjha RK, Rioja I, Taylor S, Wall ID, Watson RJ, Woolven JM, Demont EH. The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor. J Med Chem. 2020 Sep 10;63(17):9093-9126. doi: 10.1021/acs.jmedchem.0c00796. Epub 2020 Aug 30. PMID: 32702236. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.073 ml | 15.367 ml | 30.734 ml |
5 mM | 0.615 ml | 3.073 ml | 6.147 ml |
10 mM | 0.307 ml | 1.537 ml | 3.073 ml |
5 mM | 0.061 ml | 0.307 ml | 0.615 ml |
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