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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-E3 Ubiquitin Ligase-PFI-7
PFI-7

Chemical Structure : PFI-7

CAS No.: 2910938-58-6

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PFI-7 (PFI 7, PFI7)

货号: PC-22417Not For Human Use, Lab Use Only.

PFI-7 is a potent, selective and cell-active chemical probe inhibitor for GID4, a substrate-binding receptor within the C-terminal to LisH (CTLH) E3 ligase complex.

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

    生物&药学活性

    PFI-7 is a potent, selective and cell-active chemical probe inhibitor for Glucose-Induced Degradation 4 (GID4), the substrate receptor of the CTLH ubiquitin ligase complex, antagonizes Pro/N-degron binding to human GID4 with SPR Kd of 79 nM.
    PFI-7 can directly displace the Pro/N-degron peptide PGLWKS from the GID4-binding pocket in a peptide displacement assay (Kdisp=4.1 uM).
    PFI-7 binds within the β-barrel of GID4 substrate binding pocket, disrupting its interaction with the canonical Pro/N-degron peptide in cells.
    PFI-7 decreases GID4-HaloTag binding to PGLKWS-NanoLuc on human embryonic kidney 293T (HEK293T) cells with IC50 of 0.54 uM.
    PFI-7 is a suitable tool compound for use in cellular studies to interrogate GID4-mediated recruitment to the CTLH complex.
    The Pro/N-degron pathway is a recently identified pathway that recognizes N-terminal degrons containing unmodified Proline residues (Pro/N-degrons).

    物理化学性质&存储条件

    分子量 401.51
    分子式 C24H27N5O
    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

    Acetamide, N-[cis-4-(1H-benzimidazol-2-yl)cyclohexyl]-2-[(1H-indol-2-ylmethyl)amino]-

    参考文献

    1. Owens DDG, et al. Nat Chem Biol. 2024 May 21. doi: 10.1038/s41589-024-01618-0.

    2. Yazdi AK, et al. RSC Med Chem. 2024 Mar 5;15(3):1066-1071.

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