GSK 525762A

Bezeichnung:GSK 525762A

CAS-Nr1260907-17-2

Englisch Name:GSK 525762A

CBNumberCB42627926

SummenformelC22H22ClN5O2

Molgewicht423.9

MOL-Datei1260907-17-2.mol

GSK 525762A physikalisch-chemischer Eigenschaften

Schmelzpunkt	>132°C (dec.)
Dichte	1.35
storage temp.	2-8°C
Löslichkeit	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)
Aggregatzustand	powder
Farbe	white to beige
Optische Aktivität	[α]/D +80 to +90°, c = 0.3 in methanol
Stabilität	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.

Gefahreninformationscode (GHS)

GSK 525762A Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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.
Verwenden
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
Lager
Store at -20°C
Einzelnachweise
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

GSK 525762A Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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