Skepinone-LisanATP-competitive,dibenzosuberone-basedinhibitorofp38-MAPKandTNF-a,withIC50valuesof5and40nM,respectively.[1]At1000nM,Skepinone-L(Kd=1.5nM)didnotinhibitanyothermemberofanAmbitpanelof402kinases.[2]
InvitroHeLacellassaysdeterminedthatSkepinone-Lshowedaconcentration-dependentinhibitionofHSP27(Ser82)phosphorylationatanIC50of25nM.[2].FurThermore,Skepinone-Lreducedconcentrationsofwellknownp38MAPKsubstrates,suchasIL-1bandIL10(IC50=30-50nM).[2]
Technicalinformation:
| ChemicalFormula: | C24H21F2NO4 | |
| CAS#: | 1221485-83-1 | |
| MolecularWeight: | 425.42 | |
| Purity: | >99% | |
| Appearance: | Yellow | |
| ChemicalName: | (R)-2-((2,4-difluorophenyl)amino)-7-(2,3-dihydroxypropoxy)-10,11-dihydro-5H-dibenzo[a,d][7]annulen-5-one | |
| Solubility: | Upto22mMinDMSO | |
| Synonyms: | Skepinone-L |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Koeberleetal.,Design,synthesis,andBIOLOGicalevaluationofnoveldisubstituteddibenzosuberonesashighlypotentandselectiveinhibitorsofp38mitogenactivatedproteinkinase.J.Med.Chem.2012,55,5868-5877.PubmedID:22676210 |
| 2. | Koeberleetal.,Skepinone-Lisaselectivep38mitogen-activatedproteinkinaseinhibitor.Nat.Chem.Biol.2012,8,141-143.PubmedID:22198732 |
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