Skepinone-L Chemical Properties

Melting point:

130-134°C

Boiling point:

629.0±55.0 °C(Predicted)

Density 

1.384±0.06 g/cm3(Predicted)

storage temp. 

2-8°C(protect from light)

solubility 

DMSO (Slightly), Methanol (Slightly)

pka

13.49±0.20(Predicted)

form 

Solid

color 

Light Yellow to Yellow

Safety Information

HS Code 

2922500090

Skepinone-L Usage And Synthesis

Description

Skepinone-L is an ATP-competitive inhibitor of p38 MAPK isoform p38α (IC₅₀s = 5 nM) and p38β (97% inhibition at 1 μM). It has little effect on a range of other kinases, including p38γ and p38δ. Skepinone-L dose-dependently blocks the phosphorylation of heat shock protein 27 (HSP27), a p38 MAPK substrate, in response to stimulation with anisomycin in HeLa cells (IC₅₀ = 25 nM) or TNF-α in THP-1 cells. At 1 μM, it prevents phosphorylation of cytosolic phospholipase A₂ in platelets in response to collagen-related peptide or thrombin , blunting platelet secretion and aggregation.

Uses

Skepinone-L is a potent and highly selective inhibitor of p38 MAP kinase which impairs platelet activation and thrombus formation.

target

p38-MAPK

References

[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.

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