GSK 525768A

Modify Date: 2024-01-12 15:37:35

GSK 525768A Structure
GSK 525768A structure
Common Name GSK 525768A
CAS Number 1260530-25-3 Molecular Weight 423.89500
Density N/A Boiling Point N/A
Molecular Formula C22H22ClN5O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of GSK 525768A


GSK 525768A is the inactive enantiomer of GSK525762A. GSK 525768A has no activity towards BET.

 Names

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
Synonym More Synonyms

 GSK 525768A Biological Activity

Description GSK 525768A is the inactive enantiomer of GSK525762A. GSK 525768A has no activity towards BET.
Related Catalog
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.

 Chemical & Physical Properties

Molecular Formula C22H22ClN5O2
Molecular Weight 423.89500
Exact Mass 423.14600
PSA 84.89000
LogP 3.93190
Storage condition 2-8℃

 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
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  • Purity: 98.0%
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Price: $462/10mM*1mLinDMSO

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