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Technical Data
| Formula | C24H21F2NO4 |
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| 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 | |||
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* <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.) |
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Biological Activity
| Description | Skepinone-L (CBS3830) is a selective p38α-MAPK inhibitor with IC50 of 5 nM. | ||
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| 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: |
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References
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Customer Product Validation
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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 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
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.