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NACK inhibitor UM-74

Chemical Structure : NACK inhibitor UM-74

CAS No.: 2370831-06-2

NACK inhibitor UM-74

Catalog No.: PC-20217Not For Human Use, Lab Use Only.

UM-74 is a potent and specifc inhibitor of NACK (Notch activation complex kinase), directly blocks NACK recruitment to the Notch ternary complex (NTC).

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    Biological Activity

    UM-74 is a potent and specifc inhibitor of NACK (Notch activation complex kinase), directly blocks NACK recruitment to the Notch ternary complex (NTC).
    UM-74 inhibited OE19 cell growth more potently than Z271-0326 in the colony formation assays (EC50=0.52 uM).
    UM-74 treatment significantly decreased transcription of Notch target genes HES5 and CCND1.
    UM-74 also inhibited HES5 and ALDH1 gene transcription, while not affecting CCND1 mRNA expression level in OE19 cell line.
    UM-74 (15 mg/kg, i.p.) showed in vivo efficacy in the inhibition of tumor progression in the OE19 xenograft model.
    UM-74 showed improved activity than Z271-0326.

    Physicochemical Properties

    M.Wt 553.68
    Formula C28H35N5O5S
    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

    tert-butyl (4-((4-(3-(pyrrolidine-1-carbonyl)pyrazolo[1,5-a]pyridin-5-yl)piperidin-1-yl)sulfonyl)phenyl)carbamate

    References

    1. Diluvio G, et al. Mol Ther Oncolytics. 2023 Feb 22;28:307-320.

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