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PFKL activator NA-11

Chemical Structure : PFKL activator NA-11

CAS No.: 2785323-65-9

PFKL activator NA-11 (NA-11)

Catalog No.: PC-38283Not For Human Use, Lab Use Only.

PFKL activator NA-11 is a small-molecule, selective PFKL activator, inhibits the NOX2-dependent oxidative burst in neutrophils by activating the glycolytic enzyme phosphofructokinase-1 liver type (PFKL).

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    Biological Activity

    PFKL activator NA-11 is a small-molecule, selective PFKL activator, inhibits the NOX2-dependent oxidative burst in neutrophils by activating the glycolytic enzyme phosphofructokinase-1 liver type (PFKL).
    NA-11 binds to the AMP/ADP allosteric activation site, inhibits NOX2-dependent NETosis induced by PMA with IC50 of 4 nM.
    NA-11 does not inhibit NETosis by directly modifying the enzymatic activity of NAMPT.
    NA-11 relieved inhibition of PFKL by ATP (3.1 mM) with EC50 of 14 nM in in vitro kinase assays.
    Neutrophils treated with NA-11 had reduced NOX2-dependent outputs, including neutrophil cell death (NETosis) and tissue damage.

    Physicochemical Properties

    M.Wt 401.466
    Formula C24H23N3O3
    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

    N-[2-[2-(5-Hydroxy-1-pentyn-1-yl)phenyl]-4H,10H-pyrazolo[5,1-c][1,4]benzoxazepin-7-yl]acetamide

    References

    1. Neri Amara, et al. Cell. 2021 Aug 19;184(17):4480-4494.e15.

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