A cell-permeable naphthyridine N-oxide compound that acts as a potent, reversible p38α MAP kinase inhibitor (IC₅₀ = 68 nM) and exhibits excellent selectivity among 54-kinases. It acts on the ATP-binding site plus an adjacent hydrophobic pocket. Exhibits desirable ADME (Absorption, Distribution, Metabolism, and Excretion) profile with good microsomal stability, low toxicity, and low reactivity towards cytochrome P450 isozymes. Shown to inhibit lipopolysaccharide-induced TNFα production in a dose-dependent manner (ED₅₀ of 0.5 mg/kg).

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Lumeras, W., et al. 2011. J. Med. Chem.54, 7899.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)