KYA1797K-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEKYA1797KCat.No.:HY-101090CASNo.:1956356-56-1分⼦式:C₁₇H₁₁KN₂O₆S₂分⼦量:442.51作⽤靶点:Wnt;β-catenin作⽤通路:StemCell/Wnt储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:6mg/mL(13.56mM;Needultrasonic)H2O:1mg/mL(2.26mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2598mL11.2992mL22.5984mL5mM0.4520mL2.2598mL4.5197mL10mM0.2260mL1.1299mL2.2598mL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(sealedstorage,awayfrommoisture)。-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。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:1mg/mL(2.26mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:1mg/mL(2.26mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性KYA1797K有效，选择性的Wnt/β-catenin抑制剂，IC50值为0.75µM。IC50&TargetIC50:0.75(Wnt/β-catenin)[1]体外研究KYA1797KbindsdirectlytotheregulatorsofG-proteinsignalingdomainofaxin,initiatingb-cateninandRasdegradationthroughenhancementoftheb-catenindestructioncomplexactivatingGSK3b.KYA1797KeffectivelysuppressesthegrowthofCRCsharboringAPCandKRASmutations.KYA1797Kenhancesformationoftheβ-catenindestructioncomplexandinducedGSK3βactivation,leadingtophosphorylationofbothβ-cateninandK-RasatS33/S37/T41andT144/T148.KYA1797Kdegradesbothβ-cateninandRasSW480,LoVo,DLD1andHCT15cellsinadose-dependentmanner.KYA1797Kdestabilizesβ-cateninandRasinDLD1cellsexpressingWTβ-cateninorWTK-Ras[1].体内研究KYA1797KsignificantlysuppressestumorgrowthandprogressionbothinmousexenograftsofCRCcellsharboringAPCandK-RasmutationsandinanApcmin/+/KrasG12DLA2mousemodel.KYA1797Kadministration(25mg/kg)reducesbothweightandvolumeofthetumorby70%.KYA1797Ktreatmentsignificantlyreduceslevelsofβ-cateninandRasproteinsaswellasWnt/β-cateninandRassignalingtarget[1].PROTOCOLCellAssay[1]SW480,LoVo,DLD1andHCT15cellsaretreatedwithKYA1797K(0.2,1,5,25µM)for24hor4d.MTTassayisusedtodetermineeffectsofKYA1797Koncellproliferation[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice:KYA1797K(20mg/kg)isinjectedintraperitoneally(i.p.)intomicecarryingxenograftedtumorsfromtheAdministration[1]D-MTcelllinethatharborsbothAPCandKRASmutationsfor28days.Tumorweightismeasuredattimeofsacrificeandtumorvolumesofmicearemeasuredevery4d[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•CellDeathDis.2020Aug18;11(8):644.•CellDeathDis.2019Sep12;10(9):681.•JNeuroinflammation.2021Oct13;18(1):229.•BiomedPharmacother.2020Mar;123:109807.•LifeSci.2021Jan1;264:118726.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].ChaPH,etal.Small-moleculebindingoftheaxinRGSdomainpromotesβ-cateninandRasdegradation.NatChemBiol.2016Aug;12(8):593-600.McePdfHeightCaution:Productha