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Pipinib

Chemical Structure : Pipinib

CAS No.: 2380013-55-6

Pipinib

Catalog No.: PC-73078Not For Human Use, Lab Use Only.

Pipinib is a small molecule Hedgehog signaling inhibitior by selective inhibition of phosphatidylinositol 4-kinase IIIβ (PI4KB, IC50=2.2 uM), inhibits Purmorphamine-induced osteogenesis with IC50 of 0.6 uM.

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    Biological Activity

    Pipinib is a small molecule Hedgehog signaling inhibitior by selective inhibition of phosphatidylinositol 4-kinase IIIβ (PI4KB, IC50=2.2 uM), inhibits Purmorphamine-induced osteogenesis with IC50 of 0.6 uM.
    Pipinib inhibited GLI reporter gene activity in Sonic hedgehog (Shh)-LIGHT2 cells (IC50=1.7 uM) and expression of Hh target genes Ptch1 and Gli1 (IC50=3.1 uM and 4.1 uM, respectively).
    Pipinib does not modulate Hh signaling via SMO.
    Pipinib is an ATP-competitive inhibitor of PI4KB activity, does not inhibit isoenzymes PI4KA, PI4K2A or PI4K2B up to 50 uM.
    Pipinib suppresses GLI-mediated transcription and Hh target gene expression by impairing SMO translocation to the cilium.

    Physicochemical Properties

    M.Wt 342.417
    Formula C17H18N4O2S
    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

    Methyl 4-((2-(isopropylamino)thieno[3,2-d]pyrimidin-4-yl)amino)benzoate

    References

    1. Kremer L,, et al. Angew Chem Int Ed Engl. 2019 Nov 11;58(46):16617-16628.

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