SKF-86002 dihydrochloride

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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.

SKF-86002 dihydrochloride Chemical Structure

CAS No. : 116339-68-5

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Other In-stock Forms of SKF-86002 dihydrochloride:

SKF-86002

Other Forms of SKF-86002 dihydrochloride:

SKF-86002 In-stock

2 Publications Citing Use of MCE SKF-86002 dihydrochloride

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•Related Small Molecules:

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

Biological Activity
Purity & Documentation
References
Customer Review

Description

In Vitro

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.

Western Blot Analysis^[4]

Cell Line:	U937 cells
Concentration:	10 μM
Incubation Time:	72 hours
Result:	Reduced CD23 levels on IL-4-treated U937 cells.

In Vivo

SKF-86002 dihydrochloride (10-90 mg/kg; p.o.; daily; for 22 days) has antiarthritic activity^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Lewis rats, with adjuvant-induced arthritis (AA)^[5]
Dosage:	10 mg/kg, 30 mg/kg, 90 mg/kg
Administration:	Oral administration, daily, for 22 days
Result:	Significantly decreased hindleg volumes after injection of adjuvant.

Molecular Weight

370.27

Formula

C₁₆H₁₄Cl₂FN₃S

CAS No.

116339-68-5

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

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]