Skepinone-L

Catalog No.S7214 Batch:S721402

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Technical Data

Formula

C24H21F2NO4
Molecular Weight 425.42 CAS No. 1221485-83-1
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)
Homogeneous suspension
0.5% methylcellulose
10.0mg/ml Taking the 1 mL working solution as an example, take 10 mg of this product, add it to 1 ml of 0.5% methylcellulose clear solution, and mix evenly to form a uniform suspension. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Skepinone-L (CBS3830) 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 (from reference)

Animal Study:

[1]
  • Animal Models

    Mice

  • Dosages

    ~3 mg/kg

  • Administration

    Oral administration

Customer Product Validation

Data from [Data independently produced by , , Cell Physiol Biochem,2015, 36(2):631-641.]

Selleck's Skepinone-L has been cited by 9 publications

Cellular stress induces non-canonical activation of the receptor tyrosine kinase EphA2 through the p38-MK2-RSK signaling pathway [ J Biol Chem, 2023, S0021-9258(23)00341-1] PubMed: 37059179
A CRISPRi/a platform in human iPSC-derived microglia uncovers regulators of disease states [ Nat Neurosci, 2022, 25(9):1149-1162] PubMed: 35953545
Alternative splicing of apoptosis genes promotes human T cell survival [ Elife, 2022, 11e80953] PubMed: 36264057
DUSP4 protects BRAF- and NRAS-mutant melanoma from oncogene overdose through modulation of MITF [ Life Sci Alliance, 2022, 5(9)e202101235] PubMed: 35580987
Elucidation of cGMP-dependent induction of mitochondrial biogenesis through PKG and p38 MAPK in the kidney. [ Am J Physiol Renal Physiol, 2020, 318(2):F322-F328] PubMed: 31841384
Phenotype-Based Screens with Conformation-Specific Inhibitors Reveal p38 Gamma and Delta as Targets for HCC Polypharmacology. [ Mol Cancer Ther, 2019, 18(9):1506-1519] PubMed: 31213506
GADD45β loss ablates innate immunosuppression in cancer [Verzella D Cancer Res, 2018, 78(5):1275-1292] PubMed: 29279355
Lab-Attenuated Rabies Virus Causes Abortive Infection and Induces Cytokine Expression in Astrocytes by Activating Mitochondrial Antiviral-Signaling Protein Signaling Pathway [ Front Immunol, 2017, 8:2011] PubMed: 29403485
Curcumin Modulates Macrophage Polarization Through the Inhibition of the Toll-Like Receptor 4 Expression and its Signaling Pathways [Zhou Y, et al. Cell Physiol Biochem, 2015, 36(2):631-641] PubMed: 25998190

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.