
Description | JW55isapotentandselectiveinhibitorofthecanonicalWntpathwaythatfunctionsviainhibitionofthePARPdomainoftankyrase1andtankyrase2(TNKS1/2). | |
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Targets |
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Invitro | JW55inhibitsthePARPdomainofTNKS1/2,leADIngtothestABIlizationofAXIN2followedbyincreaseddegradationofβ-catenin.Wnt3a-inducedHEK293cellscontainingatransientlytransfectedST-Luc(SuperTop-luciferase)reportershowinhibitionbyJW55withanIC50valueof470nmol/L.JW55decreasesauto-PARsylationofTNKS1/2invitrowithIC50valuesof1.9μmol/Land830nmol/L,respectively.JW55-mediatedinhibitionofcanonicalWntsignalingresultsinreducedcell-cycleprogression,proliferation,andcolonyformationintheCRCcelllineSW480invitro[1]. | |
Invivo | JW55reducesXWnt8-inducedaxisduplicationinXenopusembryosandtamoxifen-inducedpolyposisformationinconditionalAPCmutantmice[1]. |
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