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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Ubiquitin-conjugating Enzyme (E2)-DI-404
DI-404

Chemical Structure : DI-404

CAS No.: 2187412-79-7

DI-404 (DI404)

货号: PC-63182Not For Human Use, Lab Use Only.

DI-404 is a highly potent, peptidomimetic inhibitor of DCN1-UBC12 protein-protein interaction that bind to DCN1 protein with Kd of 6.9 nM, selectively inhibits the neddylation of cullin 3 over other cullin members.

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

    生物&药学活性

    DI-404 is a highly potent, peptidomimetic inhibitor of DCN1-UBC12 protein-protein interaction that bind to DCN1 protein with Kd of 6.9 nM, selectively inhibits the neddylation of cullin 3 over other cullin members.
    DI-404 effectively enhances the thermal stability of cellular DCN1 protein at 0.3 uM in H2170 cells, decreases the association of cellular DCN1 protein with cellular UBC12 protein in a dose-dependent manner.
    DI-404 effectively increases the level of NRF2 protein, a substrate of cullin 3 CRL (CRL3), but has no effect on CDT1, a substrate of cullin 4A CRL (CRL4A).

    物理化学性质&存储条件

    分子量 713.291
    分子式 C35H45ClN6O6S
    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

    (S)-6-Amino-2-((S)-2-((S)-3-(6-chlorobenzo[d]thiazol-2-yl)-2-propionamidopropanamido)-2-(tetrahydro-2H-pyran-4-yl)-acetamido)-N-((R)-chroman-4-yl)hexanamide

    参考文献

    1. Zhou H, et al. J Med Chem. 2018 Mar 8;61(5):1934-1950.

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