Skepinone-L (Synonyms: Skepinone L) |
Catalog No.GC13578 |
An inhibitor of p38 MAPK
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1221485-83-1
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Skepinone-L is a selective inhibitor of p38 mitogen-activated protein kinase (MAPK) with IC50 value of 5 nM[1].
P38 MAPKs are a class of MAPK which are responsive for stress stimuli, such as heat shock and osmotic shock. They are involved in cell differentiation and apoptosis [1].
Skepinone-L is a ATP-competitive inhibitor of p38 MAPK [1]. For in vitro test, the phosphory¬lation of heat shock protein 27 (HSP27) of the p38 MAPK pathway can be used as a marker to assess the activity of p38 MAPK. When HeLa cells were treated with anisomycin, skepinone-L showed dose-dependent inhibition of HSP27 phosphorylation with a cellular IC50 ~25 nM, which confirmed the inhibition of p38 MAPK. Additionally, in peripheral blood mononuclear cells (hPBMCs), treatment of skepinone-L resulted in the reduction of p38 MAPK downstream effectors including TNF-α, IL-1β and IL-10 [1].
In mouse model, oral administration of skepinone-L resulted in very high level of skepinone-L which was 240 nM and higher than the human whole-blood IC50 value of skepinone. Therefore, it resulted in the inhibition of TNF-α by 77% via the inhibition of upstream p38 MAPK. Thus, it demonstrated the pre¬eminent pharmacodynamic properties of skepinone-L [1].
Reference:
[1]. Koeberle, S C et al., Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor. Nature Chemical Biology, 2012, 8(2), 141-143.
Cas No. | 1221485-83-1 | SDF | |
Synonyms | Skepinone L | ||
Chemical Name | 3-(2,4-difluoroanilino)-9-[(2R)-2,3-dihydroxypropoxy]-5,6-dihydrodibenzo[3,1-[7]annulen-11-one | ||
Canonical SMILES | C1CC2=C(C=CC(=C2)NC3=C(C=C(C=C3)F)F)C(=O)C4=C1C=CC(=C4)OCC(CO)O | ||
Formula | C24H21F2NO4 | M.Wt | 425.42 |
Solubility | ≥ 21.25 mg/mL in DMSO, ≥ 46.5 mg/mL in EtOH with ultrasonic | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.3506 mL | 11.7531 mL | 23.5062 mL |
5 mM | 0.4701 mL | 2.3506 mL | 4.7012 mL |
10 mM | 0.2351 mL | 1.1753 mL | 2.3506 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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