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AS2795440

Chemical Structure : AS2795440

CAS No.: 2171506-45-7

AS2795440 (AS 2795440, AS-2795440)

Catalog No.: PC-60992Not For Human Use, Lab Use Only.

AS2795440 is a potent, selective, 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=2 nM).

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

    Biological Activity

    AS2795440 is a potent, selective, 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=2 nM).
    AS2795440 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.
    AS2795440 reduces Akt phosphorylation in IFNγ/LPS-stimulated RAW264.7 cells.
    AS2795440 greatly increases cell size with many small vesicles in the cytoplasm; prevents the development of arthritis in rats.

    Physicochemical Properties

    M.Wt 480.62
    Formula C29H32N6O
    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-(1''-isopropyl-6-methyl-1'',2'',3'',6''-tetrahydro-[3,3':6',4''-terpyridin]-5-yl)-2,3-dimethyl-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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