Name: Skepinone-L
Price: 483.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    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].
- Properties
  - Alternative Name
    
    Skepinone L; 3-(2,4-difluoroanilino)-9-[(2R)-2,3-dihydroxypropoxy]-5,6-dihydrodibenzo[3,1-[7]annulen-11-one
    
    CAS Number
    
    1221485-83-1
    
    Molecular Formula
    
    C24H21F2NO4
    
    Molecular Weight
    
    425.42
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥21.25 mg/mL in DMSO; insoluble in H2O; ≥46.5 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 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

Skepinone-L

Skepinone-L

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