| Bioactivity | SKF-86002 is an orally active p38 MAPK inhibitor, with anti-inflammatory, anti-arthritic and analgesic activities. SKF-86002 inhibits lipopolysaccharide (LPS)-stimulate human monocyte IL-1 and TNF-α production (IC50 = 1 μM). SKF-86002 inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid[1][2][3]. | ||||||||||||
| Invitro | SKF-86002 (10 μM; 1 hour) inhibits apoptosis induced by stress stimulation with UV irradiation (UV)[1].SKF-86002 does not inhibit UV-induced apoptosis in undifferentiated HL-60 cells[1].SKF-86002 (10 μM; 72 hours) prevent IL-4-induced monocyte or U937 cell CD23 surface expression and protein formation with no effect on CD23 mRNA levels[4]. Western Blot Analysis[4] Cell Line: | ||||||||||||
| In Vivo | SKF-86002 (10-90 mg/kg; p.o.; daily; for 22 days) has antiarthritic activity[5]. Animal Model: | ||||||||||||
| Name | SKF-86002 | ||||||||||||
| CAS | 72873-74-6 | ||||||||||||
| Formula | C16H12FN3S | ||||||||||||
| Molar Mass | 297.35 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Frasch SC, et al. p38 mitogen-activated protein kinase-dependent and -independent intracellular signal transduction pathways leading to apoptosis in human neutrophils. J Biol Chem. 1998 Apr 3;273(14):8389-97. [2]. Griswold DE, et al. SK&F 86002: a structurally novel anti-inflammatory agent that inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid. Biochem Pharmacol. 1987 Oct 15;36(20):3463-70. [3]. Lee JC, et al. A protein kinase involved in the regulation of inflammatory cytokine biosynthesis. Nature. 1994;372(6508):739-746. [4]. L A Marshall, et al. Inhibitors of the p38 mitogen-activated kinase modulate IL-4 induction of low affinity IgE receptor (CD23) in human monocytes. J Immunol. 1998 Dec 1;161(11):6005-13. [5]. M J DiMartino, et al. Pharmacologic characterization of the antiinflammatory properties of a new dual inhibitor of lipoxygenase and cyclooxygenase. Agents Actions. 1987 Feb;20(1-2):113-23. |