PTK7-β-catenin-IN-1-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEPTK7/β-catenin-IN-1Cat.No.:HY-160488CASNo.:906147-24-8分子式:C₂₂H₁₆N₂O₂分子量:340.37作用靶点:β-catenin作用通路:StemCell/Wnt储存方式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfromlight)溶解性数据体外实验DMSO:60mg/mL(176.28mM;Needultrasonic)SolventMass1mg5mg10mgConcentration制备储备液1mM2.9380mL14.6899mL29.3798mL5mM0.5876mL2.9380mL5.8760mL10mM0.2938mL1.4690mL2.9380mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存方式和期限：-80°C,6months;-20°C,1month(protectfromlight)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。BIOLOGICALACTIVITY生物活性PTK7/β-catenin-IN-1(compound01065)是一种有效的PTK7/β-catenin抑制剂，对PTK7/β-catenin和p53/MDM2的IC50值分别为8.9μM和56.5μM。PTK7/β-catenin-IN-1具有用于癌症研究的潜力。体外研究PTK7/β-catenin-IN-1(compound01065;72h)hasantiproliferativepropertiesinHCT116,SW480andMEFswithIC50sof19.6µM,21.3µM,41µM,respectively[1].PTK7/β-catenin-IN-1(25µM;24h)increasedthepercentageofHCT116andSW480cellsinSphasewith1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEsubsequentdecreaseinG0/G1phasessuggestingSphasearrestthatinhibitscellcycleprogression[1].PTK7/β-catenin-IN-1(25µM;24h)causesasignificantincreaseinp21andp27proteinlevels[1].PTK7/β-catenin-IN-1(25µM;24h)causessignificantreductioninAXIN2mRNAlevelinHCT116andSW480[1].CellCycleAnalysis[1]CellLine:HCT116andSW480cellsConcentration:25µMIncubationTime:24hResult:Inducedanobviouscellcyclearrestthroughdistinctmechanisms.IncreasedthepercentageofHCT116andSW480cellsinSphasewithsubsequentdecreaseinG0/G1phasessuggestingSphasearrestthatinhibitscellcycleprogression.WesternBlotAnalysis[1]CellLine:HCT116andSW480cellsConcentration:25µMIncubationTime:24hResult:Causedasignificantincreaseinp21andp27proteinlevels.RT-PCR[1]CellLine:HCT116andSW480cellsConcentration:25µMIncubationTime:24hResult:CausedasignificantreductioninAXIN2mRNAleve.REFERENCESLaetitiaGanier,etal.DiscoveryofSmall-MoleculeInhibitorsofthePTK7/β-CateninInteractionTargetingtheWntSignalingPathwayinColorectalCancer.ACSChemBiol.2022May20;17(5):1061-1072.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchu