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HPK1 PROTAC SS44

Chemical Structure : HPK1 PROTAC SS44

CAS No.: 2636072-58-5

HPK1 PROTAC SS44 (HPK1 degrader SS44)

Catalog No.: PC-72307Not For Human Use, Lab Use Only.

HPK1 PROTAC SS44 is a heterobifunctional small molecule HPK1 PROTAC degrader based on ZYF0033 that simultaneously binds HPK1 and E3 ligase Cereblon (CRBN), induces degradation of HPK1.

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    Biological Activity

    HPK1 PROTAC SS44 is a heterobifunctional small molecule HPK1 PROTAC degrader based on ZYF0033 that simultaneously binds HPK1 and E3 ligase Cereblon (CRBN), induces degradation of HPK1.
    SS44 (100 nM) caused significant degradation of HPK1 within 12 h after SS44 treatment in human PBMCs withno significant IKZF1/3 degradation, which could be blocked by treatment with the proteasome inhibitor MG132 and with the NEDD8-activating enzyme (NAE) inhibitor MLN4924.
    SS44 showed markedly stronger inhibition of tumor growth, significantly enhanced the antitumor efficacy of anti-PD-1 antibody treatment.

    Physicochemical Properties

    M.Wt 875.054
    Formula C48H54N6O8S
    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-((10-(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)-10-oxodecyl)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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