Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemENSC668394Cat.No.:HY-115492CASNo.:382605-72-3分?式:C??H??Br?N?O?分?量:452.1作?靶點(diǎn):Others作?通路:Others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:3.85mg/mL(8.52mM;ultrasonicandwarmingandheatto80°C)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.2119mL11.0595mL22.1190mL5mM0.4424mL2.2119mL4.4238mL10mM---------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?。BIOLOGICALACTIVITY?物活性NSC668394?種有效的ezrin(Thr567)磷酸化抑制劑，Kd值為12.59μM。NSC668394主通過與ezrin結(jié)合來抑制PKCΙ導(dǎo)致的ezrinT567磷酸化。NSC668394可?于預(yù)防腫瘤轉(zhuǎn)移。體外研究NSC668394(10μM;pretreatedfor15min)inhibitsezrinT567phosphorylation(IC50=8.1μM)andactinbindinginvitro[1].1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemENSC668394(1-10μM;2-6h)inhibitsezrin-mediatedinvasionbyK7M2osteosarcoma(OS)cellsontheHUVECmonolayer[1].NSC668394(20μM)causessignificantdecreaseingrowthinJM1andJM2rathepatomacelllines[2].NSC668394(10μM)reducescellmotilityphenotypesinzebrafish[1].WesternBlotAnalysis[1]CellLine:K7M2OScellsConcentration:10μMIncubationTime:6hoursResult:InhibitedT567phosphorylationandactinbindingofendogenousezrinwithoutalteringcellularezrinlevels.體內(nèi)研究NSC668394(0.226mg/kg/day;i.p.5-daysaweek)inhibitsezrin-dependentinvivoOSmetastaticgrowthinmouselung[1].AnimalModel:FemaleBALB/candSCID/BeigemicewereinjectedwithK7M2orMNNG-HOStumorcells[1]Dosage:0.226mg/kg/dayAdministration:I.p.5-daysaweekfor66daysResult:Showedanincreaseinsurvival.Decreasedthenumberofthegreenfluorescentprotein(GFP)-expressingmetastaticfociinthelungtissues.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?ResearchSquarePreprint.2021Oct.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].BulutG,et,al.Smallmoleculeinhibitorsofezrininhibittheinvasivephenotypeofosteosarcomacells.Oncogene.2012Jan19;31(3):269-81.[2].XueY,et,al.PhosphorylatedEzrin(Thr567)RegulatesHippoPathwayandYes-AssociatedProtein(Yap)inLiver.AmJPathol.2020Jul;190(7):1427-1437.[3].?elikH,et,al.EzrinInhibitionUp-regulatesStressResponseGeneExpression.JBiolChem.2016Jun17;291(25):13257-70.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapplications.For