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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Deubiquitinase (DUB)-WEHI-092
WEHI-092

Chemical Structure : WEHI-092

CAS No.: 883494-13-1

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WEHI-092 (WEHI092)

货号: PC-26500Not For Human Use, Lab Use Only.

WEHI-092 is a potent and selective inhibitor of USP9X with IC50 of 254 nM, directly binds to USP9X catalytic domain with SPR KD of 1 uM, does not inhibit USP24 and other DUBs.

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

    生物&药学活性

    WEHI-092 is a potent and selective inhibitor of USP9X with IC50 of 254 nM, directly binds to USP9X catalytic domain with SPR KD of 1 uM, does not inhibit USP24 and other DUBs.
    Incubation of the USP9X catalytic domain with 50 µM WEHI-092 inhibited cleavage of K48-linked di-ubiquitin and prevented the modification of USP9X with ubiquitin propargylamide (Ub-PA), a suicide substrate that covalently modifies the catalytic Cys1566 of USP9X.
    WEHI-092 (50 uM) does not affect any of 49 human DUBs with the exception of USP9X.
    WEHI-092 binds within the Fingers subdomain of USP9X.
    WEHI-092 is cytotoxic in a small subset of cancer cell lines, destabilises the centrosomal protein CEP55 with IC50 of 1.3 uM.
    WEHI-092 is non-lethal and non-toxic to the non-cancerous human cell lines studied (HUVECs and HDFs).
    WEHI-092 (10 uM) caused 50% cell growth inhibition, including stalling cell growth completely in MOLT-4 and SK-MEL-2 cells.
    WEHI-092 (10 uM) also led to reduced protein levels of CEP55, MKRN2, CEP131 and PCM1, in MDA-MB-231 cells.
    WEHI-092 caused arrested mitosis in MDA-MB-231, MiaPaca2, and SK-MEL-2 cells.

    物理化学性质&存储条件

    分子量 455.53
    分子式 C23H25N3O5S
    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

    (4-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)sulfonyl)piperazin-1-yl)(2,3-dimethyl-1H-indol-5-yl)methanone

    参考文献

    1. Schenk P, et al. Global analysis of cancer cell responses to USP9X inhibition. EMBO J. 2026 Apr 7. doi: 10.1038/s44318-026-00742-y.

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