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JQ1 (+)

Inh 1268524-70-4 (6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetic acid 1,1-dimethylethyl ester
Catalog No. ABIN7233264
  • Application
    Inhibition (Inh)
    Purpose
    Bromodomain inhibitor
    Characteristics
    JQ1 (+) is a potent BET bromodomain inhibitor and is the active isomer. IC50 = 17.7, 32.6, 76.9 and 12942 nM respectively for BRD2 (N-terminal (N)), BRD4 (C-terminal (C)), BRD4 (N) and CREBBP respectively (data for + isomer). Competitive binding by JQ1 displaces the BRD4 fusion oncoprotein from chromatin, prompting squamous differentiation and specific antiproliferative effects in BRD4-dependent cell lines and patient-derived xenograft models. Induces squamous differentiation in NMC cell lines and inhibits tumor growth in NMC xenografts. Displays reversible contraceptive effects in male mice. Blocks inflammation and bone loss in periodontitis. Reverses CAR T cell extinction.
    Purity
    >98 %
    Chemical Name
    (6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetic acid 1,1-dimethylethyl ester
    Formula
    C23H25ClN4O2S
    Solubility
    Soluble in DMSO (up to 60 mg/ml) or in Ethanol (up to 46 mg/ml)
  • Restrictions
    For Research Use only
  • Format
    Powder
    Precaution of Use
    GHS – Classification
    Not a hazardous substance or mixture
    Storage
    RT
  • Background
    Epigenetics,Proliferation,Bromodomain,Inflammation,Cancer,Posttranslational modification,Chromatin
    Molecular Weight
    457.0
    CAS-No
    1268524-70-4
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