1. MAPK/ERK Pathway
  2. p38 MAPK
  3. 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.

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SKF-86002 dihydrochloride

SKF-86002 dihydrochloride 構造式

CAS 番号 : 116339-68-5

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製品説明

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].

体外実験

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.
体内実験

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.
分子量

370.27

分子式

C16H14Cl2FN3S

CAS 番号
SMILES

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

純度とドキュメンテーション
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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製品名:
SKF-86002 dihydrochloride
製品番号:
HY-108641
数量:
MCE 日本正規代理店: