Skepinone-L is a selective inhibitor of p38 mitogen-activated protein kinase (MAPK) with IC50 value of 5 nM.
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 .
Skepinone-L is a ATP-competitive inhibitor of p38 MAPK . 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 .
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 .
. Koeberle, S C et al., Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor. Nature Chemical Biology, 2012, 8(2), 141-143.
- 1. Zhang XH, Li CY, et al. "Pro-angiogenic activity of isoliquiritin on HUVECs in vitro and zebrafish in vivo through Raf/MEK signaling pathway." Life Sci. 2019 Apr 15;223:128-136. PMID:30876941
- 2. Lv, Dan, et al. "Neuronal MHC Class I Expression Is Regulated by Activity Driven Calcium Signaling." PloS one 10.8 (2015): e0135223. PMID:26263390
|Physical Appearance||A solid|
|Storage||Store at -20°C|
|Solubility||≥21.25 mg/mL in DMSO, ≥46.5 mg/mL in EtOH with ultrasonic, <2.17 mg/mL in H2O|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For 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.|
|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.|
|IC50||5 nM||40 nM|
Quality Control & MSDS
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