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I-BET762

Inh 1260907-17-2 (4S)- 6-(4-Chlorophenyl)-N-ethyl-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine-4-acetamide
Catalog No. ABIN7233261
  • Application
    Inhibition (Inh)
    Purpose
    BET Bromodomain inhibitor, Suppresses Myc transcription
    Characteristics
    I-BET762 is a potent inhibitor of the BET family of bromodomains with no activity at bromodomains BAZ2B, SP140, ATAD2, CREBBO, and PCAF. 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 mice, and suppressed the inflammatory function of T cells. Inhibition of BET bromodomains results in downregulation of Myc transcription, an important oncogene.
    Purity
    >98 %
    Chemical Name
    (4S)- 6-(4-Chlorophenyl)-N-ethyl-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine-4-acetamide
    Formula
    C22H22ClN5O2
    Solubility
    Soluble in DMSO (up to at least 25 mg/ml) or in Ethanol (up to at least 25 mg/ml)
  • Restrictions
    For Research Use only
  • Format
    Powder
    Precaution of Use
    GHS – Classification
    Not a hazardous substance or mixture
    Storage
    -20 °C
  • Background
    GSK525762,Epigenetics,Bromodomain,Immunology,Inflammation,Cancer,Posttranslational modification,Chromatin
    Molecular Weight
    423.90
    CAS-No
    1260907-17-2
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