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    Skepinone-L (CBS3830)
    Skepinone-L (CBS3830)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0486
    CAS #: 1221485-83-1Purity ≥98%

    Description: Skepinone-L (CBS-3830; CBS3830) is a novel, potent, selective and ATP-competitive inhibitor p38α-MAPK with potential anti-inflammatory activity. It inhibits p38α-MAPK with an IC50 of 5 nM.  

    References: Nat Chem Biol. 2011 Dec 25;8(2):141-3; Cell Physiol Biochem. 2013;31(6):914-24.

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    Molecular Weight (MW)425.42
    FormulaC24H21F2NO4
    CAS No.1221485-83-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 85 mg/mL (199.8 mM)
    Water: <1 mg/mL
    Ethanol: 85 mg/mL (199.8 mM)
    Solubility (In vivo)0.5% methylcellulose: 30 mg/mL
    SynonymsSynonym: CBS3830; CBS-3830; CBS 3830; Skepinone-L

    Chemical Name: 2-[(2,4-difluorophenyl)amino]-7-[(2R)-2,3-dihydroxypropoxy]-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-one

    InChi Key: HXMGCTFLLWPVFM-GOSISDBHSA-N

    InChi Code: InChI=1S/C24H21F2NO4/c25-16-4-8-23(22(26)10-16)27-17-5-7-20-15(9-17)2-1-14-3-6-19(11-21(14)24(20)30)31-13-18(29)12-28/h3-11,18,27-29H,1-2,12-13H2/t18-/m1/s1

    SMILES Code: O=C1C2=CC=C(NC3=CC=C(F)C=C3F)C=C2CCC4=CC=C(OC[[email protected]](O)CO)C=C14


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    In Vitro

    In vitro activity: Skepinone-L shows concentration-dependent inhibition of HSP27 (Ser82) phosphorylation through the p38 MAPK pathway with a cellular IC50 of approximately 25 nM, and also reduces concentrations of TNF-α, IL-1β and IL-10, regulated by p38 MAPK, with IC50 ranging from 30 to 50 nM. Skepinone-L (1 μM) abrogates the phosphorylation of platelet p38 MAPK substrate Hsp27 activated by stimulation with CRP, thrombin or thromboxane A2 analogue U-46619, and impairs platelet secretion and aggregation.


    Kinase Assay: Skepinone-L (CBS3830), the first ATP-competitive p38 MAPK inhibitor with excellent in vivo efficacy and selectivity. Therefore, Skepinone-L (CBS3830) is a valuable probe for chem. biol. research, and it may foster the development of a unique class of kinase inhibitors.

    In VivoIn 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.
    Animal modelMouse
    Formulation & DosageDissolved in methyl cellulose; 3 mg/kg; p.o.
    References

    Nat Chem Biol. 2011 Dec 25;8(2):141-3; Cell Physiol Biochem. 2013;31(6):914-24.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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