1260530-25-3

1260530-25-3 structure

Name: GSK 525768A
Chemical Name: 2-[(4R)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide
CAS Number: 1260530-25-3
Molecular Formula: C₂₂H₂₂ClN₅O₂
Molecular Weight: 423.89500
Catalog: Research Areas Cancer
Create Date: 2016-04-25 19:35:08
Modify Date: 2024-01-12 15:37:35
GSK 525768A is the inactive enantiomer of GSK525762A. GSK 525768A has no activity towards BET.

Name	2-[(4R)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide
Synonyms	2-[(4R)-6-(4-chlorophenyl)-1-methyl-8-(methyloxy)-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide CS-1255 GSK 525768A

Description	GSK 525768A is the inactive enantiomer of GSK525762A. GSK 525768A has no activity towards BET.
Related Catalog	Signaling Pathways >> Others >> Others Research Areas >> Cancer
In Vitro	GSK 525768A has no activity towards BET[1]. 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[2].
References	[1]. Nicodeme E, et al. Suppression of inflammation by a synthetic histone mimic. Nature. 2010 Dec 23;468(7327):1119-23. [2]. Filippakopoulos P, et al. Targeting bromodomains: epigenetic readers of lysine acetylation. Nat Rev Drug Discov. 2014 May;13(5):337-56.