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AS2677131

Chemical Structure : AS2677131

CAS No.: 2171502-44-4

AS2677131 (AS 2677131;AS-2677131)

Catalog No.: PC-60991Not For Human Use, Lab Use Only.

AS2677131 is a novel potent, oral PIKfyve inhibitor that selectively decreases c-Rel binding to gene promoters of IL-12p40 and IL-1β, regulates cytokine production through PIKfyve-c-Rel pathway ( IL-12p40 IC50=4 nM).

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    Biological Activity

    AS2677131 is a novel potent, oral PIKfyve inhibitor that selectively decreases c-Rel binding to gene promoters of IL-12p40 and IL-1β, regulates cytokine production through PIKfyve-c-Rel pathway ( IL-12p40 IC50=4 nM).
    AS2677131 inhibits the production of IL-12p40, IL-6 and IL-1β but not TNFα in activated macrophages or dendritic cells, and expression of IgM-induced MHC class II on B cells.
    AS2677131 reduces Akt phosphorylation in IFNγ/LPS-stimulated RAW264.7 cells.
    AS2677131 greatly increases cell size with many small vesicles in the cytoplasm.

    Physicochemical Properties

    M.Wt 470.577
    Formula C27H30N6O2
    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

    rel-N-{6'-[(2R,6S)-2,6-dimethylmorpholin-4-yl]-3,3'-bipyridin-5-yl}-3-ethyl-2-methyl-1H-pyrrolo[3,2-b]pyridine-5-carboxamide

    References

    1. Terajima M, et al. Eur J Pharmacol. 2016 Jun 5;780:93-105.

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