中文名 | GSK 525768A |
英文名 | GSK 525768A |
别名 | 化合物 T11472 BROMODOMAIN抑制剂(GSK 525768A) |
英文别名 | GSK525768A GSK-525768 GSK-525768A GSK 525768A GSK-525768A (4R)-6-(4-Chlorophenyl)-N-ethyl-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine-4-acetamide 4H-[1,2,4]Triazolo[4,3-a][1,4]benzodiazepine-4-acetamide, 6-(4-chlorophenyl)-N-ethyl-8-methoxy-1-methyl-, (4R)- |
CAS | 1260530-25-3 |
化学式 | C22H22ClN5O2 |
分子量 | 423.9 |
密度 | 1.35±0.1 g/cm3(Predicted) |
熔点 | 140-145℃ |
溶解度 | 10毫米DMSO |
酸度系数 | 15.71±0.46(Predicted) |
存储条件 | -20℃ |
体外研究 | GSK 525768A has no activity towards BET. GSK 525768A (GSK525768A) is the (R)-enantiomer of GSK525762A. GSK525762A is shown to regulate levels of the high-density lipid protein apolipoprotein A1 (APOA1) in assays monitoring APOA1 release in liver cells, whereas the (R)-enantiomer (GSK 525768A) has no effect. GSK 525768A directly engages the protein module by forming hydrogen bonds with the conserved asparagine residue in a way that mimics the binding mode of acetylated lysine; this usually results in the binding of the inhibitor deeper within the acetylated lysine binding site but without displacing the conserved water molecules that are present at the bottom of the acetyl-lysine binding cavity. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.359 ml | 11.795 ml | 23.591 ml |
5 mM | 0.472 ml | 2.359 ml | 4.718 ml |
10 mM | 0.236 ml | 1.18 ml | 2.359 ml |
5 mM | 0.047 ml | 0.236 ml | 0.472 ml |
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