Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEKYA1797KCat.No.:HY-101090CASNo.:1956356-56-1分?式:C??H??KN?O?S?分?量:442.51作?靶點(diǎn):Wnt;β-catenin作?通路:StemCell/Wnt儲(chǔ)存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:6mg/mL(13.56mM;Needultrasonic)H2O:1mg/mL(2.26mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.2598mL11.2992mL22.5984mL5mM0.4520mL2.2598mL4.5197mL10mM0.2260mL1.1299mL2.2598mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:1mg/mL(2.26mM);Suspendedsolution;Needultrasonic2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:1mg/mL(2.26mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性KYA1797K有效，選擇性的Wnt/β-catenin抑制劑，IC50值為0.75μM。IC50&TargetIC50:0.75(Wnt/β-catenin)[1]體外研究KYA1797KbindsdirectlytotheregulatorsofG-proteinsignalingdomainofaxin,initiatingb-cateninandRasdegradationthroughenhancementoftheb-catenindestructioncomplexactivatingGSK3b.KYA1797KeffectivelysuppressesthegrowthofCRCsharboringAPCandKRASmutations.KYA1797Kenhancesformationoftheβ-catenindestructioncomplexandinducedGSK3βactivation,leadingtophosphorylationofbothβ-cateninandK-RasatS33/S37/T41andT144/T148.KYA1797Kdegradesbothβ-cateninandRasSW480,LoVo,DLD1andHCT15cellsinadose-dependentmanner.KYA1797Kdestabilizesβ-cateninandRasinDLD1cellsexpressingWTβ-cateninorWTK-Ras[1].體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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?邊的抑制劑?師www.MedChemEREFERENCES[1].ChaPH,etal.Small-moleculebindingoftheaxinRGSdomainpromotesβ-cateninandRasdegradation.NatChemBiol.2016Aug;12(8):593-600.McePdfHeightCaution:Productha