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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

Quick Overview for JQ1 (+) (ABIN7233264)

Application

Inhibition (Inh)

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
  • 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 %

    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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