SKF86002

SKF86002 (CAS No.: 72873-74-6) is a small-molecule, orally active inhibitor of p38 mitogen-activated protein kinase (MAPK) with well-characterized anti-inflammatory, anti-arthritic, and analgesic properties, widely used as a pharmacological tool in inflammation and signal transduction research. It modulates inflammatory signaling by suppressing p38 MAPK-dependent pathways and by inhibiting lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid, thereby reducing the production of key eicosanoids and pro-inflammatory mediators. In cellular systems, SKF86002 effectively attenuates lipopolysaccharide-induced cytokine release, including interleukin-1 and tumor necrosis factor-α, in human monocytes at low micromolar concentrations, and also inhibits prostanoid and leukotriene biosynthesis across immune cell types. In addition, it demonstrates activity against prostaglandin H2 synthase and reduces inflammatory mediator production in both human and rodent cells. In vivo, SKF86002 has been shown to alleviate inflammation and tissue swelling in rodent models of arthritis and to improve survival in models of endotoxic shock, consistent with its ability to suppress systemic cytokine responses. This compound is commonly applied in studies investigating MAPK signaling, cytokine regulation, and inflammatory disease mechanisms, as well as in preclinical drug discovery efforts targeting immune and inflammatory pathways, with experimental concentrations or dosing regimens varying depending on specific model systems and study objectives.