I-BET762, BET Bromodomain inhibitor; Suppresses Myc transcription (TBI4122)

Description

Product Details

Formal Name: (4S)- 6-(4-Chlorophenyl)-N-ethyl-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine-4-acetamide

Alternate Names: GSK525762

Molecular Formula: C₂₂H₂₂ClN₅O₂

Formula Weight: 423.90

CAS Number: 1260907-17-2

Purity: >98%

Formulation: powder

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

Storage: -20°C

Stability: ≥ 1 year.

Applications

BET Bromodomain inhibitor; Suppresses Myc transcription

Functions

I-BET762 is a potent inhibitor of the BET family of bromodomains with no activity at bromodomains BAZ2B, SP140, ATAD2, CREBBO, and PCAF.1,2 IC50’s for H4Ac peptide displacement: BRD2 = 32.5nM, BRD3 = 42.4nM, BRD4 = 36.1nM. It was able to suppress proinflammatory proteins by macrophage, block acute inflammation in mice1, and suppressed the inflammatory function of T cells. Inhibition of BET bromodomains results in downregulation of Myc transcription, an important oncogene.

Application Procedures

First dissolved in DMSO (up to at least 25 mg/ml) or in Ethanol (up to at least 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.