Skepinone-L

For research use only.

Catalog No.S7214

4 publications

Skepinone-L Chemical Structure

CAS No. 1221485-83-1

Skepinone-L is a selective p38α-MAPK inhibitor with IC50 of 5 nM.

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Selleck's Skepinone-L has been cited by 4 publications

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  • TLR4/MAPK pathway regulated macrophage polarization towards M1 phenotype. LPS/INF-γ induced macrophages were cultured in the absence or presence of siTLR4, SP600125(an inhibitor of JNK), SCH772984(an inhibitor of ERK) and Skepinone-L(an inhibitor of p38) respectively for 24h. Then, all the cells were harvested for western blot assay.

    Cell Physiol Biochem,2015, 36(2):631-641.. Skepinone-L purchased from Selleck.

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Choose Selective p38 MAPK Inhibitors

Biological Activity

Description Skepinone-L is a selective p38α-MAPK inhibitor with IC50 of 5 nM.
Targets
p38α [1]
5 nM
In vitro

Skepinone-L shows concentration-dependent inhibition of HSP27 (Ser82) phosphorylation through the p38 MAPK pathway with a cellular IC50 of approximately 25 nM, and also reduces concentrations of TNF-α, IL-1β and IL-10, regulated by p38 MAPK, with IC50 ranging from 30 to 50 nM . [1] Skepinone-L (1 μM) abrogates the phosphorylation of platelet p38 MAPK substrate Hsp27 activated by stimulation with CRP, thrombin or thromboxane A2 analogue U-46619, and impairs platelet secretion and aggregation. [2]
In vivo In vivo, skepinone-L inhibits Gal/ LPS-induced TNF-α release by 77%. [1]

Protocol

Animal Research:

[1]
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  • Animal Models: Mice
  • Dosages: ~3 mg/kg
  • Administration: Oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 85 mg/mL (199.8 mM)
Ethanol 85 mg/mL (199.8 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% methylcellulose
For best results, use promptly after mixing. 		30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 425.42
Formula

C24H21F2NO4
CAS No. 1221485-83-1
Storage powder
in solvent
Synonyms N/A
Smiles C1CC2=C(C=CC(=C2)NC3=C(C=C(C=C3)F)F)C(=O)C4=C1C=CC(=C4)OCC(CO)O

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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p38 MAPK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID