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HPK1 PROTAC SS47

Chemical Structure : HPK1 PROTAC SS47

CAS No.: 2636072-62-1

HPK1 PROTAC SS47 (HPK1 degrader SS47)

Catalog No.: PC-72308Not For Human Use, Lab Use Only.

HPK1 PROTAC SS47 is a heterobifunctional small molecule based on ZYF0033 that simultaneously binds HPK1 and E3 ligase Cereblon (CRBN), induces degradation of HPK1.

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    Biological Activity

    HPK1 PROTAC SS47 is a heterobifunctional small molecule HPK1 degrader based on ZYF0033 that simultaneously binds HPK1 and E3 ligase Cereblon (CRBN), induces degradation of HPK1.
    SS47 exerts proteasome-mediated HPK1 degradation within 48 h of treatment, SS47 (100 nM) induced HPK1 degradation in bone-marrow-derived DCs, significantly increased the proliferation of CD4+ and CD8+ T cells and the secretion of IFN-γ.
    SS47 showed markedly better inhibition of tumor growth than either ZYF0033 or the ddH2O control in mice with subcutaneous 4T-1 tumors.

    Physicochemical Properties

    M.Wt 953.077
    Formula C49H56N6O12S
    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

    4-((15-(4-(5-(6-amino-5-((3-(3-hydroxy-3-methylbut-1-yn-1-yl)benzyl)oxy)pyridin-3-yl)thiazol-2-yl)piperidin-1-yl)-15-oxo-3,6,9,12-tetraoxapentadecyl)oxy)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione

    References

    1. Jingwen Si, et al. Cancer Cell. 2020 Oct 12;38(4):551-566.e11.

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