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首页-小分子抑制剂&激动剂-Wnt/Notch/Hedgehog-Notch-Z271-0326
Z271-0326

Chemical Structure : Z271-0326

CAS No.: 1243002-72-3

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Z271-0326 (Z 271-0326)

货号: PC-20216Not For Human Use, Lab Use Only.

Z271-0326 is a first-in-class, potent and specifc inhibitor of NACK (Notch activation complex kinase) with SPR KD value of 0.89 uM, directly blocks NACK recruitment to the Notch ternary complex (NTC).

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

    生物&药学活性

    Z271-0326 is a first-in-class, potent and specifc inhibitor of NACK (Notch activation complex kinase) with SPR KD value of 0.89 uM, directly blocks NACK recruitment to the Notch ternary complex (NTC).
    Z271-0326 enhanced the NACK ATPase activity in a manner dependent on the ATP concentration.
    Z271-0326 displayed a dose-dependent reduction in colony formation in both OE19 (EC50=3.6 μM) and OE33 (EC50=3.14 μM) cell lines.
    Z271-0326 inhibited NACK, Notch1, and MAML1 binding to DNA-bound CSL (CBF-1/RBP-J, Su(H), Lag-1), whereas no effect was observed in CSL binding to DNA.
    Z271-0326 significantly inhibited the transcription of Notch target genes in both OE19 and OE33 cell lines, inhibited proliferation by causing cell-cycle arrest and apoptosis in esophageal adenocarcinoma.
    Z271-0326 (15 mg/kg, i.p.) showed in vivo efficacy in the inhibition of tumor progression in the OE19 xenograft model.

    物理化学性质&存储条件

    分子量 497.61
    分子式 C25H31N5O4S
    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

    5-(1-((4-acetamidophenyl)sulfonyl)piperidin-4-yl)-N,N-diethylpyrazolo[1,5-a]pyridine-3-carboxamide

    参考文献

    1. Diluvio G, et al. Mol Ther Oncolytics. 2023 Feb 22;28:307-320.

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