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Skepinone-L (Synonyms: Skepinone L)

Catalog No.GC13578

An inhibitor of p38 MAPK

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Skepinone-L Chemical Structure

Cas No.: 1221485-83-1

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10mM (in 1mL DMSO)
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5mg
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10mg
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50mg
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200mg
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Sample solution is provided at 25 µL, 10mM.

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Quality Control & SDS

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Background

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.

Chemical Properties

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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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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