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SMURF1 inhibitor 38

Chemical Structure : SMURF1 inhibitor 38

CAS No.: 1824708-03-3

SMURF1 inhibitor 38

Catalog No.: PC-20904Not For Human Use, Lab Use Only.

SMURF1 inhibitor 38 is a potent, specific E3 ubiquitin protein ligase 1 (SMURF1) inhibitor with biochemical IC50 of 92 nM, displays no activity against SMURF2.

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    Biological Activity

    SMURF1 inhibitor 38 is a potent, specific E3 ubiquitin protein ligase 1 (SMURF1) inhibitor with biochemical IC50 of 92 nM, displays no activity against SMURF2.
    SMURF1 inhibitor 38 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 38 shows a clean safety pharmacology profile against a standard panel of ion channels and GPCRs.
    SMURF1 inhibitor 38 (10 mg/kg) exhibits in vivo efficacy in the hypoxia/Sugen rat model of pulmonary hypertension.

    Physicochemical Properties

    M.Wt 468.99
    Formula C24H29ClN6O2
    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-(2-chloro-4-cyclopropylphenyl)-N-(2-cyclohexyl-1,5-dimethyl-3-oxo-2,3-dihydro-1H-pyrazol-4-yl)-5-methyl-1H-1,2,3-triazole-4-carboxamide

    References

    1. Duncan E Shaw, et al. J Med Chem. 2023 Jun 22;66(12):8130-8139.

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