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HPK1 inhibitor 1

Chemical Structure : HPK1 inhibitor 1

CAS No.: 2246358-08-5

HPK1 inhibitor 1

Catalog No.: PC-72013Not For Human Use, Lab Use Only.

HPK1 inhibitor 1 is a highly potent, selective inhibitor of HPK1/MAP4K1 with biochemical IC50 of 0.0465 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    HPK1 inhibitor 1 is a highly potent, selective inhibitor of HPK1/MAP4K1 with biochemical IC50 of 0.0465 nM.
    HPK1 inhibitor 1 displays >100-fold selectivity against 260 kinases in a panel of 265 kinases.
    HPK1 inhibitor 1 decreased SLP-76 phosphorylation in a human pSLP-76 ELISA at an IC50 lower than 0.02 uM.
    HPK1 inhibitor 1 enhanced Th1 cytokine production in T cells and fully reverted immune suppression imposed by the prostaglandin E2 (PGE2) and adenosine pathways in human T cells.
    HPK1 inhibitor 1 demonstrated a synergistic effect, resulting in enhanced interferon (IFN)-γ production when combination with pembrolizumab in human PBMCs

    Physicochemical Properties

    M.Wt 474.544
    Formula C25H27FN8O
    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

    2-((8-amino-6-(5-amino-4-methylpyridin-3-yl)-7-fluoroisoquinolin-3-yl)amino)-6-isopropyl-5,6-dihydro-4H-pyrazolo[1,5-d][1,4]diazepin-7(8H)-one

    References

    1. Brian M Lacey, et al. SLAS Discov. 2021 Jan;26(1):88-99.

    2. Yun Wang, et al. PLoS One. 2020 Dec 3;15(12):e0243145.

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