≥98%(HPLC) , 1260907-17-2

Synonym(s):
;(4S)- 6-(4-Chlorophenyl)-N-ethyl-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine-4-acetamide;A;I-BET

CAS NO.：1260907-17-2

Empirical Formula: C22H22ClN5O2

Molecular Weight: 423.9

MDL number: MFCD22417091

Pack Size	Price	Stock	Quantity
5mg	RMB1293.00	In Stock
25mg	RMB5219.44	In Stock
others			Enquire

Update time: 2022-07-08

PRODUCT 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)
form	powder
pka	15.71±0.46(Predicted)
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.

Description and Uses

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.

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.