Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEWnt-C59Cat.No.:HY-15659CASNo.:1243243-89-1Synonyms:C59分?式:C??H??N?O分?量:379.45作?靶點(diǎn):Porcupine;Wnt作?通路:StemCell/Wnt儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:50mg/mL(131.77mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.6354mL13.1770mL26.3539mL5mM0.5271mL2.6354mL5.2708mL10mM0.2635mL1.3177mL2.6354mL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。-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?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/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%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(6.59mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.59mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.59mM);ClearsolutionBIOLOGICALACTIVITY?物活性Wnt-C59(C59)?效可?服的PORCN抑制劑，IC50為74pM。IC50&TargetIC50:74pM(PORCN)[1]體外研究Wnt-C59(C59)inhibitsPORCNactivityinvitroatnanomolarconcentrations,asassessedbyinhibitionofWntpalmitoylation,WntinteractionwiththecarrierproteinWntless/WLS,Wntsecretion,andWntactivationofβ-cateninreporteractivity.Wnt-C59inhibitsWNT3A-mediatedactivationofamultimerizedTCF-bindingsitedrivingluciferasewithanIC50of74pM[1].體內(nèi)研究Wnt-C59displaysgoodbioavailabilityinmice.Wnt-C59blocksprogressionofmammarytumorsinMMTV-WNT1transgenicmicewhiledownregulatingWnt/β-catenintargetgenes[1].Wnt-C59hasthepotentialtoeradicatecancerstemcellsinhumantumors.Wnt-C59inhibitsstemnesspropertiesofNPCcellsinadosage-dependentmannerbyarrestingsphereformationinbothHNE1andSUNE1cells[2].PROTOCOLCellAssay[2]1×104HK1,CNE1,HNE1andSUNE1cellsareseededin24-wellplates,andWnt-C59(5μM,10μM,and20μM)isaddedthenextday.Cellconfluenceisdeterminedbymicroscopyat24,48,72,and96hoursafterseedingofcells.TheIC50isdeterminedbyMTTassay[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice[1]Administration[1]FemalenudemiceorthotopicallytransplantedwithindependentMMTV-WNT1tumorsaretreatedwithvehicleorWnt-C5910mg/kgoncedailyfor17days.Tumorvolumesaremeasuredonalternatedays[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?JExpClinCancerRes.2020Jan28;39(1):22.?JExpClinCancerRes.2020Jan28;39(1):22.?MolTher-NuclAcids.2021May28.?FrontImmunol.2021Mar15;12:619209.?JMedGenet.2022Jun14;jmedgenet-2021-108396.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].ProffittKD,etal.PharmacologicalinhibitionoftheWntacyltransferasePORCNpreventsgrowthofWNT-drivenmammarycancer.CancerRes.2013Jan15;73(2):502-7.[2].ChengY,etal.Wnt-C59arrestsstemnessandsuppressesgrowthofnasopharyngealcarcinomainmicebyinhibitingtheWntpathwayinthetumormicroenvironment.Oncotarget.2015Jun10;6(16):14428-39.McePdfHeightCaution:Producthasnot