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WDR5 inhibitor 41

Chemical Structure : WDR5 inhibitor 41

CAS No.: 2417012-26-9

WDR5 inhibitor 41

Catalog No.: PC-38521Not For Human Use, Lab Use Only.

WDR5 inhibitor 41 is a potent, selective and orally bioavailable WDR5 WIN-site inhibitor with TR-FRET Ki value of <0.02 nM, inhibits cell proliferation of MV4:11 and MOLM-13 with IC50 of 13 and 27 nM, respectively.

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    Biological Activity

    WDR5 inhibitor 41 is a potent, selective and orally bioavailable WDR5 WIN-site inhibitor with TR-FRET Ki value of <0.02 nM, inhibits cell proliferation of MV4:11 and MOLM-13 with IC50 of 13 and 27 nM, respectively.
    WDR5 inhibitor 41 is well tolerated in mice by both iv and po dosing and showed no clinical sign of abnormalities suggesting an enhanced safety
    profile for the series.

    Physicochemical Properties

    M.Wt 534.587
    Formula C29H29F3N6O
    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)-7-((1H-imidazol-1-yl)methyl)-2-(cyclopropyl(4-methylpyridin-2-yl)methyl)-5-(1-ethyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)-3,4-dihydroisoquinolin-1(2H)-one

    References

    1. Kevin B. Teuscher, et al. J Med Chem. 2022. DOI: 10.1021/acs.jmedchem.2c00195

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