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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
产品编号 ABIN7233264
发货至: 中国

Quick Overview for JQ1 (+) (ABIN7233264)

应用范围

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
  • 原理

    Bromodomain inhibitor

    产品特性

    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.

    纯度

    >98 %

    Formula

    C23H25ClN4O2S

    Solubility

    Soluble in DMSO (up to 60 mg/ml) or in Ethanol (up to 46 mg/ml)
  • 限制

    仅限研究用
  • 状态

    Powder

    注意事项

    GHS – Classification
    Not a hazardous substance or mixture

    储存条件

    RT
  • 背景

    Epigenetics,Proliferation,Bromodomain,Inflammation,Cancer,Posttranslational modification,Chromatin

    分子量

    457.0

    CAS-编号

    1268524-70-4
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