Molecular Formula | C24H21F2NO4 |
Molar Mass | 425.42 |
Density | 1.384±0.06 g/cm3(Predicted) |
Melting Point | 130-134°C |
Boling Point | 629.0±55.0 °C(Predicted) |
Solubility | DMSO (Slightly), Methanol (Slightly) |
Appearance | Solid |
Color | Light Yellow to Yellow |
pKa | 13.49±0.20(Predicted) |
Storage Condition | 2-8°C(protect from light) |
In vitro study | Skepinone-L showed a concentration-dependent inhibition of HSP27 (Ser82) phosphorylation through the p38 MAPK pathway, the intracellular IC50 was about 25 nM, and it was also able to reduce TNF-α regulated by p38 MAPK, concentrations of IL-1β and IL-10, IC50 ranged from 30 to 50 nM. Skepinone-L (1 μm) abrogates the phosphorylation of the platelet p38 MAPK substrate Hsp27 activated by CRP, thrombin, or thromboxane A2 analog U-46619 stimulation, while also impairing platelet secretion and aggregation. |
In vivo study | In Vivo, skepinone-L inhibited the Gal/LPS-induced release of TNF-α by 77%. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.351 ml | 11.753 ml | 23.506 ml |
5 mM | 0.47 ml | 2.351 ml | 4.701 ml |
10 mM | 0.235 ml | 1.175 ml | 2.351 ml |
5 mM | 0.047 ml | 0.235 ml | 0.47 ml |
biological activity | Skepinone-L is a selective p38 MAPK inhibitor with an IC50 of 5 nM. Skepinone-L (CBS3830) is a selective p38 MAPK inhibitor with an IC50 of 5 nM. |
Target | Value |
p38α | 5 nM |