Antibodies
Skepinone-L
- 貨號 Cat. No.
- S7214
- 規格 Size
- 5mgã€25mg
- 品牌 Brand
- Selleckchem
Description
Skepinone-L
Catalog No.S7214
Skepinone-L is a selective p38α-MAPK inhibitor with IC50 of 5 nM.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | Skepinone-L is a selective p38α-MAPK inhibitor with IC50 of 5 nM. | |||||
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| Targets | p38α-MAPK | |||||
| IC50 | 5 nM [1] | |||||
| 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] | |||||
| Features | ||||||
Protocol(Only for Reference)
Kinase Assay: [1]
| Cell-free p38α-MAPK activity assay | 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. |
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Animal Study: [1]
| Animal Models | Mice |
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| Dosages | ~3 mg/kg |
| Administration | Oral administration |
| Solubility | 0.5% methylcellulose, 30 mg/mL |
References
Chemical Information
| Molecular Weight (MW) | 425.42 |
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| Formula | C24H21F2NO4 |
| CAS No. | 1221485-83-1 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 85 mg/mL (199 mM) |
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| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | 85 mg/mL (199 mM) | ||
| In vivo | 0.5% methylcellulose, | 30 mg/mL | |
| * <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. | |||
| Chemical Name | 5H-Dibenzo[a,d]cyclohepten-5-one, 2-[(2,4-difluorophenyl)amino]-7-[(2R)-2,3-dihydroxypropoxy]-10,11-dihydro- |
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