GSK 525762A Chemical Properties

Melting point:

>132°C (dec.)

Density 

1.35

storage temp. 

2-8°C

solubility 

Soluble in DMSO (up to at least 25 mg/ml) or in Ethanol (up to at least 25 mg/ml)

pka

15.71±0.46(Predicted)

form 

powder

color 

white to beige

optical activity

[α]/D +80 to +90°, c = 0.3 in methanol

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.

GSK 525762A Usage And Synthesis

Description

The bromodomain and extra terminal domain (BET) family of proteins, including BRD2, BRD3, and BRD4, affect inflammatory gene expression by controlling the assembly of histone acetylation-dependent chromatin complexes. I-BET762 is a synthetic compound which interacts with BET proteins with high-affinity (K_d = 32.5-42.5 nM). It blocks binding of BET proteins with acetylated histones, disrupting the formation of chromatin complexes involved in the expression of specific inflammatory genes in activated macrophages. Through these actions, I-BET762 provides protection against bacteria-induced sepsis and lipopolysaccharide-triggered endotoxic shock.

Uses

GSK 525762A, is a BET Bromodomain Inhibitor, which is now in clinical development. BET bromodomains have emerged as promising drug targets for treatment of cancers, inflammatory diseases, and other medical conditions.

Definition

ChEBI: 2-[(4S)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide is a benzodiazepine.

Biochem/physiol Actions

I-BET762 possesses anti-inflammatory property by controlling the pro-inflammatory gene expression. I-BET762 hinders the MYC (proto-oncogene) expression in cellular models. This action of I-BET762 might serve as an effective therapy in treating prostate cancer.

target

BET

storage

Store at -20°C

References

1) Nicodeme?et al.?(2010),?Suppression of inflammation by a synthetic histone mimic; Nature?468?1119 2) Mirguet?et al.?(2013),?Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains; J. Med. Chem.,?56?7501 3) Bandukwala?et al.?(2012),?Selective inhibition of CD4+ T-cell cytokine production and autoimmunity by BET protein and c-Myc inhibitors; Proc. Natl. Acad. Sci. USA,?109?14532 4) Delmore?et al.?(2011),?BET Bromodomain as a Therapeutic Strategy to Target c-Myc; Cell?146?904

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