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UBE2M-DCN1 inhibitor 52

Chemical Structure : UBE2M-DCN1 inhibitor 52

CAS No.: 2089293-14-9

UBE2M-DCN1 inhibitor 52

Catalog No.: PC-63291Not For Human Use, Lab Use Only.

UBE2M-DCN1 inhibitor 52 is a highly potent inhibitor of DCN1-UBE2M protein-protein interaction with IC50 of 60 nM, inhibits cullin neddylation in pulse-chase NEDD8 transfer assay with EC50 of 80 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    UBE2M-DCN1 inhibitor 52 is a highly potent inhibitor of DCN1-UBE2M protein-protein interaction with IC50 of 60 nM, inhibits cullin neddylation in pulse-chase NEDD8 transfer assay with EC50 of 80 nM.
    UBE2M-DCN1 inhibitor 52 binds to DCN1 and selectively reduce steady-state levels of neddylated CUL1 and CUL3 in a squamous cell carcinoma cell line.
    UBE2M-DCN1 inhibitor 52 inhibits DCN1 but not DCN3 stimulated NEDD8 transfer from UBE2F to the cullins.

    Physicochemical Properties

    M.Wt 447.546
    Formula C25H32F3N3O
    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

    1-Benzyl-1-(1-(pentan-2-yl)piperidin-4-yl)-3-(3-(trifluoromethyl)-phenyl)urea

    References

    1. Hammill JT, et al. J Med Chem. 2018 Apr 12;61(7):2680-2693.

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