Skepinone-L

For research use only.

Catalog No.S7214

4 publications

Molecular Weight(MW): 425.42

Skepinone-L is a selective p38α-MAPK inhibitor with IC50 of 5 nM.

Selleck's Skepinone-L has been cited by 4 publications

Am J Physiol Renal Physiol, 2020, 318(2):F322-F328

PubMed: 31841384 ( click the link to review the publication )

Mol Cancer Ther, 2019, 18(9):1506-1519

PubMed: 31213506 ( click the link to review the publication )

Cancer Res, 2018, 78(5):1275-1292

PubMed: 29279355 ( click the link to review the publication )

Cell Physiol Biochem, 2015, 36(2):631-641

PubMed: 25998190 ( click the link to review the publication )

1 Customer Review

TLR4/MAPK pathway regulated macrophage polarization towards M1 phenotype. LPS/INF-γ induced macrophages were cultured in the absence or presence of siTLR4, SP600125(an inhibitor of JNK), SCH772984(an inhibitor of ERK) and Skepinone-L(an inhibitor of p38) respectively for 24h. Then, all the cells were harvested for western blot assay.

Cell Physiol Biochem,2015, 36(2):631-641.. Skepinone-L purchased from Selleck.

Purity & Quality Control

Choose Selective p38 MAPK Inhibitors

Biological Activity

Description

Skepinone-L is a selective p38α-MAPK inhibitor with IC50 of 5 nM.

Targets

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] 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]

Protocol

Animal Research: ^[1]	- Collapse Animal Models: Mice Dosages: ~3 mg/kg Administration: Oral administration (Only for Reference)

References

Solubility (25°C)

In vitro	DMSO	85 mg/mL (199.8 mM)
	Ethanol	85 mg/mL (199.8 mM)
	Water	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 0.5% methylcellulose For best results, use promptly after mixing.	30 mg/mL

* 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 Information Download Skepinone-L SDF

Molecular Weight	425.42
Formula	C₂₄H₂₁F₂NO₄
CAS No.	1221485-83-1
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	N/A
Smiles	OCC(O)COC1=CC=C2CCC3=CC(=CC=C3C(=O)C2=C1)NC4=CC=C(F)C=C4F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage

mg/kg

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Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

% DMSO+ % + % Tween 80+ % ddH₂O

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Calculation results:

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 DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，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 as vortex, ultrasound or hot water bath can be used to aid dissolving.

Bio Calculators

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions
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Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
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C8=C7/X	C8:	LOG(C8):

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

p38 MAPK Signaling Pathway Map

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Skepinone-L