NCGC00378430-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemENCGC00378430Cat.No.:HY-138657CASNo.:920650-00-6分?式:C??H??N?O?S分?量:441.5作?靶點:Phosphatase作?通路:MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(226.50mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.2650mL11.3250mL22.6501mL5mM0.4530mL2.2650mL4.5300mL10mM0.2265mL1.1325mL2.2650mL請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(5.66mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.66mM);ClearsolutionBIOLOGICALACTIVITY?物活性NCGC00378430?種有效的SIX1/EYA2相互作?抑制劑。NCGC00378430部分逆轉SIX1過表達介導的轉錄和代謝譜，并逆轉SIX1誘導的TGF-β信號傳導和上?-間質轉化(EMT)。NCGC00378430在??模型中抑制SIX1介導的乳腺癌轉移。體外研究NCGC00378430isapotentSIX1/EYA2interactioninhibitorwithanIC50of52μMintheAlphascreenassay[1].NCGC00378430(20μM;3days)blocksTGF-βinducedactivationofp-Smad3,upregulationofFN1,anddownregulationofE-CADinT47Dcells[1].NCGC00378430(10μM;3days)reversestheSineoculishomeoboxhomolog1(SIX1)-inducedincreaseinp-SMAD3anddoesnotaltertotalE-CADlevels.NCGC00378430restoresmembranousE-CADinMCF7-SIX1cells,alongwithinhibitingFN1expression[1].NCGC00378430(10or20μM)disruptsSIX1-EYA2interactioninbreastcancercells(MCF7,T47D,MDA-MB-231cells)[1].NCGC00378430(10μM;for3days)partiallyreversesSIX1-mediatedtranscriptionalandmetabolicsignaturesinMCF7breasttumorcells[1].WesternBlotAnalysis[1]CellLine:T47DcellsConcentration:20μMIncubationTime:3daysResult:BlockedTGF-βinducedactivationofp-Smad3,upregulationofFN1,anddownregulationofE-CAD.體內研究NCGC00378430(25mg/kg;localinjectiontothesiteoftumor;everyotherday;fromday3untiltheday21)dramaticallydecreasesdistantmetastaticburdencomparedtovehicletreatment[1].NCGC00378430(20mg/kg;IV)hasaT1/2αof0.25hours[1].AnimalModel:6-8weekoldNSGmicewithMCF7tumorcells[1]Dosage:25mg/kgAdministration:LocalInjectiontothesiteoftumor;everyotherday;fromday3untiltheday21Result:Dramaticallydecreaseddistantmetastaticburdencomparedtovehicletreatment.Hadnogrowthinhibitoryeffect.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEAnimalModel:Mice[1]Dosage:20mg/kg(PharmacokineticAnalysis)Administration:IVResult:HadaT1/2αof0.25hours,aCLof6.19L/hr?kg,aVssof4.08L/kg,aCmaxof6703ng/mLandanAUCof3234ng/mL?hr.REFERENCES[1].HengboZhou,etal.IdentificationofaSmall-MoleculeInhibitorThatDisruptstheSIX1/EYA2Complex,EMT,andMetastasis.CancerRes.2020Jun15;80(12):2689-2702.McePdfHeightCaution:Producthasnotbeenfullyvali