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首页-小分子抑制剂&激动剂-Others-Other Targets-BJP-06-005-3
BJP-06-005-3

Chemical Structure : BJP-06-005-3

CAS No.: 2400958-08-7

BJP-06-005-3

货号: PC-72215Not For Human Use, Lab Use Only.

BJP-06-005-3 is a potent, selective, covalent, cell-permeable peptide Pin1 inhibitor (Ki=48 nM) that covalently target Cys113, a highly conserved cysteine located in the Pin1 active site.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    BJP-06-005-3 is a potent, selective, covalent, cell-permeable peptide Pin1 inhibitor (Ki=48 nM) that covalently target Cys113, a highly conserved cysteine located in the Pin1 active site.
    BJP-06–005-3 potently inhibited Pin1 catalytic activity with an apparent Ki of 48 nM in PPIase assays.
    BJP-06-005-3 reduced cell viability cross a panel of cancer cell lines in a dose- and time-dependent manner.
    BJP-06-005-3 increased phospho-CDK1 Tyr15 in Pin1-WT PDAC cell, but not in Pin1 KO cells, affected expression of downstream Pin1 substrates, increased c-Myc protein levels, cooperated with KRASG12V degradation.

    物理化学性质&存储条件

    分子量 738.283
    分子式 C37H48ClN7O7
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    ethyl (S)-2-((S)-2-((S)-1-(N-(2-chloroacetyl)-N-methyl-L-phenylalanyl)piperidine-2-carboxamido)-3-(1H-indol-3-yl)propanamido)-5-ureidopentanoate

    参考文献

    1. Benika J Pinch, et al. Nat Chem Biol. 2020 Sep;16(9):979-987.

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