受注:045-509-1970 |
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Synonyms | CBS3830 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C24H21F2NO4 |
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分子量 | 425.42 | CAS No. | 1221485-83-1 | ||||
Solubility (25°C)* | 体外 | DMSO | 85 mg/mL (199.8 mM) | ||||
Ethanol | 85 mg/mL (199.8 mM) | ||||||
Water | Insoluble | ||||||
体内 (毎回新しく調製した物を用意してください) |
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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. |
製品説明 | 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] |
キナーゼアッセイ | Cell-free p38α-MAPK activity assay | |
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Microtiter plates are coated with 50 μl of ATF-2 (10 μ/mL in TBS) for 1.5 h at 37 °C, washed with bidistilled water, blocked with blocking buffer (BB; 0.05% Tween 20, 0.25% BSA, 0,02% NaN3 in TBS) for 30 min at room temperature, and washed again. 50 μL of the respective test solution is incubated for 1 h at 37 °C. Test solutions contained 12 ng/well p38-MAPK diluted in kinase buffer (50 mM Tris, pH 7.5, 10 mM MgCl2, 10 mM β-glycerophosphate, 100 μg/mL BSA, 1 mM dithiothretiol, 0.1 mM Na3VO4, 100 μM rATP) with or without test substance (10 nM-100 μM). Test substances are dissolved in dimethyl sulfoxide to form stock solutions of 10 mM, all further dilution steps are carried out in kinase buffer. After subsequent washing, plates are blocked again with BB for 15 min followed by a washing step. 1. AB (50 μL, 1:500 in BB) was incubated for 1 h at 37 °C followed by washing and incubation with 50 μL of the 2. AB (alkaline phosphatase conjugated) (1:4000 in BB). After a final washing step, 100 μL of 4-nitrophenyl phosphate (NPP) is pipetted in each well and colour development was measured 1.5–2 h later with an enzyme-linked immunosorbent assay reader equipped with the SOFTmax PRO software at 405 nm. | ||
動物実験 | 動物モデル | Mice |
投薬量 | ~3 mg/kg | |
投与方法 | Oral administration |
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Data from [Data independently produced by , , Cell Physiol Biochem,2015, 36(2):631-641.]
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 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。