Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemELOM612Cat.No.:HY-101035CASNo.:2173232-79-4分?式:C??H??N?O?S分?量:258.3作?靶點:Others作?通路:Others儲存?式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性數據體外實驗DMSO:6mg/mL(23.23mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.8715mL19.3573mL38.7147mL5mM0.7743mL3.8715mL7.7429mL10mM0.3871mL1.9357mL3.8715mL請根據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(storedundernitrogen)。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。BIOLOGICALACTIVITY?物活性LOM612有效對FOXO胞質-胞核穿梭進?定位，在U2foxRELOC細胞中EC50值為1.5μM[1]。IC50&TargetEC50:1.5μM(FOXO,inU2foxRELOCcells)[1]體外研究LOM612potentlyactivatesnucleartranslocationofFOXOwithanEC50valueof1.5μM,andthiseffectisindependentofCRM-1.LOM612effectivelyinducestranslocationofendogenousFOXO3aandFOXO1,and1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEincreasestheexpressionoftheFOXOtargetgenesp27andFasL.LOM612showsnoeffectonthenuclearexportofendogenousNFKB2transcriptionfactorinU2OScells.LOM612iscytotoxictoHepG2cells,withanIC50valueof0.64μM,anddoesnotsensitizenon-cancerTHLE2cells(IC50,2.76μM)[1].PROTOCOLCellAssay[1]Cellsareseededataconcentrationof1×104cells/wellin200μLculturemediumandincubatedat37°Cin5%CO2.After24hours,whenthemonolayerformed,themediumisreplacedwithafinalvolumeof200μLofnewmediumwithtestedcompounds(LOM612,etc.)orcontrolsareaddedtotheplates.Cellsaretreatedwitheight2-foldserialdilutionsofeachcompoundspanningconcentrationsfrom50μMto0.39μMin1%DMSOfinal.Controlsareonthefirstandthelastcolumnsoftheplates.Onthefirstcolumn,methylmethanesulfonate(MMS)actsasapositivecontrolandDMSOasanegativecontrol.Whencompounds(LOM612,etc.)andcontrolsareadded,platesareincubatedat37°Cin5%CO2incubatorfor72hours.Afterthistime,MTTsolutionispreparedat5mg/mLinPBS1Xandthendilutedat0.5mg/mLinMEMwithoutphenolred.Thesamplesolutioninwellsisflickedoffand100μLofMTTdyeisaddedtoeachwell.Theplatesaregentlyshakenandincubatedfor3hoursat37°Cin5%CO2incubator.Thesupernatantisremovedand100μLofDMSO100%isadded.Theplatesaregentlyshakentosolubilizetheformedformazan.Theabsorbanceismeasuredatawavelengthof570nm[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].CautainB,etal.DiscoveryofaNovel,Isothiazolonaphthoquinone-BasedSmallMoleculeActivatorofFOXONuclear-CytoplasmicShuttling.PLoSOne.2016Dec9;11(12):e0167491.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedica