SKF-86002 (dihydrochloride)

SKF-86002 dihydrochloride is an orally active p38 MAPK inhibitor, with anti-inflammatory, anti-arthritic and analgesic activities. SKF-86002 dihydrochloride inhibits lipopolysaccharide (LPS) -stimulate human monocyte IL-1 and TNF-α production (IC50 = 1 μM) . SKF-86002 dihydrochloride inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid[1][2][3].

Product Specifications

CAS Number

[116339-68-5]

UNSPSC

12352005

Target

P38 MAPK

Type

Reference compound

Related Pathways

MAPK/ERK Pathway

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/skf-86002-dihydrochloride.html

Solubility

10 mM in DMSO

Smiles

[H]Cl.FC1=CC=C(C2=C(C3=CC=NC=C3)N4C(SCC4)=N2)C=C1.[H]Cl

Molecular Formula

C16H14Cl2FN3S

Molecular Weight

370.27

References & Citations

[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.