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AS3334034

Chemical Structure : AS3334034

CAS No.: 2724942-14-5

AS3334034 (AS 3334034)

Catalog No.: PC-47116Not For Human Use, Lab Use Only.

AS3334034 is a potent, selective inhibitor of the receptor-interacting protein kinase 2 (RIPK2) with IC50 of 3.02 and 2.10 nM for rat and human RIP2 kinase activity, respectively.

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    Biological Activity

    AS3334034 is a potent, selective inhibitor of the receptor-interacting protein kinase 2 (RIPK2) with IC50 of 3.02 and 2.10 nM for rat and human RIP2 kinase activity, respectively.
    AS3334034 concentration-dependently inhibited MDP-induced NF-κB activation in HCT116 cells with IC50 of 4.4 nM.
    AS3334034 displays >480-fold selectivity against a great panel of kinases, only partially inhibits several kinase activities at 1 uM, such as discoidin domain receptor and ephrin receptor.
    AS3334034 (3-30 mg/kg, p.o.) dose-dependently inhibited MDP-induced increase in plasma MCP-1 level in rats.
    AS3334034 (10 mg/kg, once daily, p.o.) significantly reduced urinary protein excretion and prevented the development of glomerulosclerosis and tubulointerstitial fibrosis in uninephrectomized adriamycin-induced CKD rats.

    Physicochemical Properties

    M.Wt 374.459
    Formula C18H22N4O3S
    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

    7-methoxy-6-(2-methylpropane-2-sulfonyl)-N-(4-methyl-1H-pyrazol-3-yl)quinolin-4-amine

    References

    1. Wada Y, et al. J Pharmacol Exp Ther. 2020 Sep;374(3):428-437.

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