中文名称:

GSK 525768A

中文同义词:

BROMODOMAIN抑制剂(GSK 525768A)

英文名称:

GSK-525768A

英文同义词:

GSK 525768A;GSK525768A;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;GSK-525768;GSK525768A; GSK-525768A;4H-[1,2,4]Triazolo[4,3-a][1,4]benzodiazepine-4-acetamide, 6-(4-chlorophenyl)-N-ethyl-8-methoxy-1-methyl-, (4R)-

CAS号:

1260530-25-3

分子式:

C22H22ClN5O2

分子量:

423.9

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

1260530-25-3.mol

熔点 

140-145℃

密度 

1.35±0.1 g/cm3(Predicted)

酸度系数(pKa)

15.71±0.46(Predicted)

生物活性

GSK 525768A 是 GSK525762A 的无活性对映体。GSK 525768A 对 BET 没有活性。

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.