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p38 MAPK-IN-4

Chemical Structure : p38 MAPK-IN-4

CAS No.: 1006378-90-0

p38 MAPK-IN-4

Catalog No.: PC-43250Not For Human Use, Lab Use Only.

p38 MAPK-IN-4 is a potent and selective inhibitor of p38 MAPK with IC50 of 68 nM for p38α, inhibits LPS-induced TNFα release in THP-1 cells with IC50 of 187 nM.

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

    Biological Activity

    p38 MAPK-IN-4 is a potent and selective inhibitor of p38 MAPK with IC50 of 68 nM for p38α, inhibits LPS-induced TNFα release in THP-1 cells with IC50 of 187 nM.
    p38 MAPK-IN-4 displays no signigicant activity against a panel of 54 tyrosine kinases and serine/threonine kinases.
    p38 MAPK-IN-4 dose-dependently inhibits TNFα production with an ED50 of 0.5 mg/kg in rat-LPS induced TNFα model, dose-dependently inhibits arthritis progression with ED50 <1 mg/kg, demonstrates a superior efficacy of 4 versus other clinically tested reference compounds like BIRB-796 and VX-745.

    Physicochemical Properties

    M.Wt 349.3534
    Formula C21H15F2N2O
    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

    1,7-Naphthyridine, 4-(2,4-difluorophenyl)-8-(2-methylphenyl)-, 7-oxide

    References

    1. Lumeras W, et al. J Med Chem. 2011 Nov 24;54(22):7899-910.

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