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SMURF1 inhibitor Cpd-6

Chemical Structure : SMURF1 inhibitor Cpd-6

CAS No.: 1824647-09-7

SMURF1 inhibitor Cpd-6 (Smurf1-IN-5)

Catalog No.: PC-20919Not For Human Use, Lab Use Only.

SMURF1 inhibitor Cpd-6 is a potent, specific E3 ubiquitin protein ligase 1 (SMURF1) inhibitor with biochemical IC50 of 11 nM, displays no activity against SMURF2.

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    Biological Activity

    SMURF1 inhibitor Cpd-6 is a potent, specific E3 ubiquitin protein ligase 1 (SMURF1) inhibitor with biochemical IC50 of 11 nM, displays no activity against SMURF2.
    SMURF1 inhibitor Cpd-6 also is highly selective against an E3 ligase panel consisting of ubiquitin-protein ligase E3A (UBE3A/E6AP), WW domain-containing protein 1/NEDD4-like E3 ubiquitin-protein ligase (WWP1), WW domain-containing protein 2 (Wwp2), neural precursor cell expressed developmentally downregulated protein 4 (Nedd4), Itch.
    SMURF1 inhibitor Cpd-6 shows a clean safety pharmacology profile against a standard panel of ion channels and GPCRs.
    SMURF1 inhibitor Cpd-6 (10 mg/kg) exhibits in vivo efficacy in the hypoxia/Sugen rat model of pulmonary hypertension.

    Physicochemical Properties

    M.Wt 480.92
    Formula C25H22ClFN4O3
    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

    5-(2-chloro-4-cyclopropylphenyl)-N-(2-(2-fluorophenyl)-1,5-dimethyl-3-oxo-2,3-dihydro-1H-pyrazol-4-yl)-4-methylisoxazole-3-carboxamide

    References

    1. Duncan E Shaw, et al. J Med Chem. 2023 Jun 22;66(12):8130-8139. 2. Rothman AMK, et al. Cell. 2025 May 15;188(10):2603-2620.e18.

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