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SKF-86002

SKU: orb1224128

Description

SKF-86002 is a potent inhibitor of p38 MAPK with IC50 of 0.5-1 uM, inhibits LPS-induced IL-1 and TNF-α production in human monocyte with IC50 of 1 uM; inhibits prostaglandin H2 (PGH2) synthase activity (IC50=120 uM) as well as prostanoid production by rat basophilic leukemia (RBL-1) cells (IC50=70 uM); blocks superoxide anion production in response to FMLP and reduces adhesion and chemotaxis in response to PAF or FMLP in human neutrophils; also inhibits 5-lipoxygenase- and cyclooxygenase-mediated arachidonic acid metabolism in RBL-1 cells (IC50=10 and 100 uM respectively), shows anti-inflammatory in vivo.

Images & Validation

Key Properties

CAS Number72873-74-6
MW297.35
Purity>98% (HPLC)
FormulaC16H12FN3S
SMILESFC1=CC=C(C2=C(C3=CC=NC=C3)N4C(SCC4)=N2)C=C1
Targetp38 MAPK
Solubility10 mM in DMSO

Bioactivity

In Vivo
Animal model: Lewis rats, with adjuvant-induced arthritis (AA). 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.
In Vitro
Western blot analysis. Cell line: U937 cells. Concentration: 10 μM. Incubation time: 72 hours. Result: Significantly reduced CD23 levels on IL-4-treated U937 cells.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

SKF86002

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Quality Guarantee

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SKF-86002 (orb1224128)

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Available Sizes

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2 mg
$ 90.00
5 mg
$ 130.00
10 mg
$ 200.00
25 mg
$ 340.00
50 mg
$ 480.00
100 mg
$ 700.00
500 mg
$ 1,460.00