SKF-86002 is a potent inhibitor of p38 MAPK with IC50 of 0.5-1 uM, inhibits LPS-induced IL-1 and TNF-α production in human monocyte with IC50 of 1 uM.
SKF-86002 inhibits prostaglandin H2 (PGH2) synthase activity (IC50=120 uM) as well as prostanoid production by rat basophilic leukemia (RBL-1) cells (IC50=70 uM).
SKF-86002 blocks superoxide anion production in response to FMLP and reduces adhesion and chemotaxis in response to PAF or FMLP in human neutrophils.
SKF-86002 also inhibits 5-lipoxygenase- and cyclooxygenase-mediated arachidonic acid metabolism in RBL-1 cells (IC50=10 and 100 uM respectively), shows anti-inflammatory in vivo.
