SKF-86002 dihydrochloride
Based on 3 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- CAS No.: 116339-68-5
- Formula: C16H14Cl2FN3S
- Molecular Weight:370.27
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) SKF-86002 dihydrochloride
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Biological Activity
SKF-86002 dihydrochloride (10 μM; 1 hour) inhibits apoptosis induced by stress stimulation with UV irradiation (UV)[1].
SKF-86002 dihydrochloride does not inhibit UV-induced apoptosis in undifferentiated HL-60 cells[1].
SKF-86002 dihydrochloride (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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U937 cells
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Concentration:10 μM
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Incubation Time:72 hours
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Result:Reduced CD23 levels on IL-4-treated U937 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Lewis rats, with adjuvant-induced arthritis (AA)[5]
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Dosage:10 mg/kg, 30 mg/kg, 90 mg/kg
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Administration:Oral administration, daily, for 22 days
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Result:Significantly decreased hindleg volumes after injection of adjuvant.
Chemical Information
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CAS No. 116339-68-5
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Molecular Weight 370.27
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Formula C16H14Cl2FN3S
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SMILES
[H]Cl.FC1=CC=C(C2=C(C3=CC=NC=C3)N4C(SCC4)=N2)C=C1.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (3)
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Journal Impact Factor
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Most Recent
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Sci Transl Med
Inhibition of p38α MAPK restores neuronal p38γ MAPK and ameliorates synaptic degeneration in a mouse model of DLB/PD. [Abstract]2023 May 10;15(695):eabq6089. PMID: 37163617 -
Stem Cells
β-Arrestin 2 and Epac2 Cooperatively Mediate DRD1-Stimulated Proliferation of Human Neural Stem Cells and Growth of Human Cerebral Organoids. [Abstract]2022 Sep 26;40(9):857-869. PMID: 35772103 -
J Stroke Cerebrovasc Dis
Blockage of p38MAPK in astrocytes alleviates brain damage in a mouse model of embolic stroke through the CX43/AQP4 axis. [Abstract]2024 Dec;33(12):108085. PMID: 39393507
Purity & Documentation
References
[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. [Content Brief]
[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. [Content Brief]
[3]. Lee JC, et al. A protein kinase involved in the regulation of inflammatory cytokine biosynthesis. Nature. 1994;372(6508):739-746. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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