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BI-2536

Inh 755038-02-9 4-[[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-7H-pteridin-2-yl]amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide
产品编号 ABIN7233234
发货至: 中国
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Quick Overview for BI-2536 (ABIN7233234)

应用范围

Inhibition (Inh)

Chemical Name

4-[[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-7H-pteridin-2-yl]amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide
  • 原理

    Dual Plk/BRD4 inhibitor, Destabilizes Myc

    产品特性

    BI 2536 was originally reported as a potent (IC50's Plk1 = 0.83nM, Plk2 = 3.5nM and Plk3 = 9.0nM) and selective2 Polo-like kinase inhibitor (IC50's Plk1 = 0.83nM, Plk2 = 3.5nM and Plk3 = 9.0nM) that caused mitotic arrest and apoptosis induction in various human cancer cell lines. It was later found to be a potent inhibitor (IC50 = 100nM) of BET family member BRD4 and able to potently suppress c-Myc expression in MM.1S multiple myeloma cells. BI 2536 destabilizes N-Myc by inhibiting the deactivation of the ubiquitin E3 ligase Fbw7 by Plk1.

    纯度

    >97 %

    Formula

    C28H39N7O3

    Solubility

    Soluble in DMSO (up to 20 mg/ml) or in Ethanol (up to 25 mg/ml)
  • 限制

    仅限研究用
  • 状态

    Powder

    储存条件

    -20 °C
  • 背景

    Apoptosis inducer,Epigenetics,Cell cycle,Myc,Bromodomain,Ubiquitin/Proteasome,Cell death,Cancer,Posttranslational modification,Chromatin

    分子量

    521.67

    CAS-编号

    755038-02-9
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