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Poloppin

Chemical Structure : Poloppin

CAS No.: 683808-78-8

Poloppin

Catalog No.: PC-61200Not For Human Use, Lab Use Only.

Poloppin is a cell-active, small molecule inhibitor of protein-protein interaction via the Polo-box domain (PBD) of the mitotic Polo-like kinase (PLK) with IC50 of 26.9 uM (PLK1) in FP assays.

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    Biological Activity

    Poloppin is a cell-active, small molecule inhibitor of protein-protein interaction via the Polo-box domain (PBD) of the mitotic Polo-like kinase (PLK) with IC50 of 26.9 uM (PLK1) in FP assays.
    Poloppin triggers dose-dependent mitotic arrest with non-congressed chromosomes in human cell lines, preferentially kills cells expressing mutant KRAS (SW48 G12D GI50=5.2 uM, SW48 Wt GI50=13.7 uM).
    Poloppin sensitizes mutant KRAS-expressing cells to clinical inhibitors of c-MET.

    Physicochemical Properties

    M.Wt 438.244
    Formula C20H15BrF3NO2
    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

    3-(5-(4-bromophenyl)-1-(2-(trifluoromethyl)phenyl)-1H-pyrrol-2-yl)propanoic acid

    References

    1. Narvaez AJ, et al. Cell Chem Biol. 2017 Aug 17;24(8):1017-1028.e7.

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