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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Deubiquitinase (DUB)-HY041004
HY041004

Chemical Structure : HY041004

CAS No.: 2412899-25-1

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HY041004 (HY 041004)

货号: PC-21610Not For Human Use, Lab Use Only.

HY041004 is the first small molecule inhibitor of deubiquitinase Josephin Domain-containing protein 2 (JOSD2) with IC50 of 0.26 uM for JOSD2 catalytic activity inhibition.

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

    生物&药学活性

    HY041004 is the first small molecule inhibitor of deubiquitinase Josephin Domain-containing protein 2 (JOSD2) with IC50 of 0.26 uM for JOSD2 catalytic activity inhibition.
    HY041004 (2 uM) shows potent inhibitory effect against JOSD2 catalytic activity as 86.14% in in vitro ubiquitin-AMC assays, also robustly blocks the loss of K6-linked polyubiquitination on LKB1 caused by JOSD2 in cellular assays.
    HY041004 also exhibits on-target engagement in cancer cells in cellular thermal shift assay.
    HY041004 displays a less but comparable inhibition on JOSD1 (IC50=0.47 μM) and much weaker activity against other two MJDs Ataxin-3 and Ataxin-3L with IC50 of 5.4 and 12.8 μM, respectively.
    HY041004 displays potent anticancer effects in NSCLC cell in vitro, which is dependent on JOSD2-LKB1 axis.
    HY041004 (orally, twice daily, 50 mg/kg and 100 mg/kg) significantly suppresses tumor growth and induced intratumor cell apoptosis on NCI-H1299 xenografted tumors.

    物理化学性质&存储条件

    分子量 342.71
    分子式 C16H8ClFN4O2
    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

    3-(3-chloro-5-fluorobenzyl)-3H-[1,2,3]triazolo[4,5-g]isoquinoline-4,9-dione

    参考文献

    1. Liu, J. et al. The invention discloses a naphthoquinone triazole core skeleton derivative compound, a preparation method and application thereof. China patent CN110218198A (2019).

    2. Tao Yuan, et al. Signal Transduct Target Ther. 2024 Jan 5;9(1):11.

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