LOM612-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELOM612Cat.No.:HY-101035CASNo.:2173232-79-4分⼦式:C₁₃H₁₀N₂O₂S分⼦量:258.3作⽤靶点:Others作⽤通路:Others储存⽅式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性数据体外实验DMSO:6mg/mL(23.23mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.8715mL19.3573mL38.7147mL5mM0.7743mL3.8715mL7.7429mL10mM0.3871mL1.9357mL3.8715mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(storedundernitrogen)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。BIOLOGICALACTIVITY⽣物活性LOM612有效对FOXO胞质-胞核穿梭进⾏定位，在U2foxRELOC细胞中EC50值为1.5μM[1]。IC50&TargetEC50:1.5μM(FOXO,inU2foxRELOCcells)[1]体外研究LOM612potentlyactivatesnucleartranslocationofFOXOwithanEC50valueof1.5μM,andthiseffectisindependentofCRM-1.LOM612effectivelyinducestranslocationofendogenousFOXO3aandFOXO1,and1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师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