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GSK 525768A

CAS No. : 1260530-25-3

MCE 站：GSK 525768A

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

研究领域：Others

作用靶点：Others

In Vitro: 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.

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