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Skepinone-L p38 MAPK inhibitor

Cat.No.S7214

Skepinone-L (CBS3830) is a selective p38α-MAPK inhibitor with IC50 of 5 nM.
Skepinone-L p38 MAPK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 425.42

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 425.42 Formula

C24H21F2NO4

Storage (From the date of receipt)
CAS No. 1221485-83-1 Download SDF Storage of Stock Solutions

Synonyms CBS3830 Smiles C1CC2=C(C=CC(=C2)NC3=C(C=C(C=C3)F)F)C(=O)C4=C1C=CC(=C4)OCC(CO)O

Solubility

In vitro
Batch:

DMSO : 85 mg/mL (199.8 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 85 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Mechanism of Action

Targets/IC50/Ki
p38α [1]
5 nM
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] This compound (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]
References

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