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Skepinone-L

In stock
Catalog No.
A3824
P38-MAPK inhibitor,potent and selective
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$315.00
In stock
5mg
$287.00
In stock
10mg
$369.00
In stock
50mg
$997.00
In stock
200mg
$2,262.00
In stock

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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.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt425.42
Cas No.1221485-83-1
FormulaC24H21F2NO4
SynonymsSkepinone L
Solubility≥21.25 mg/mL in DMSO, ≥46.5 mg/mL in EtOH with ultrasonic, <2.17 mg/mL in H2O
Chemical Name3-(2,4-difluoroanilino)-9-[(2R)-2,3-dihydroxypropoxy]-5,6-dihydrodibenzo[3,1-[7]annulen-11-one
SDFDownload SDF
Canonical SMILESC1CC2=C(C=CC(=C2)NC3=C(C=C(C=C3)F)F)C(=O)C4=C1C=CC(=C4)OCC(CO)O
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description Skepinone-L is a selective inhibitor of p38 mitogen-activated protein kinase (MAPK) and TNF-α with IC50 values of 5 nM and 40 nM, respectively.
Targets p38-MAPK TNF-α        
IC50 5 nM 40 nM        

Quality Control

Chemical structure

Skepinone-L

Related Biological Data

Skepinone-L

Related Biological Data

Skepinone-L

Related Biological Data

Skepinone-L