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DI-404

Chemical Structure : DI-404

CAS No.: 2187412-79-7

DI-404 (DI404)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    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).

    Physicochemical Properties

    M.Wt 713.291
    Formula C35H45ClN6O6S
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    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

    References

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

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