Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEEN4Cat.No.:HY-134761CASNo.:1197824-15-9分?式:C??H??N?O?分?量:416.47作?靶點:c-Myc作?通路:Apoptosis儲存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數(shù)據(jù)體外實驗DMSO:250mg/mL(600.28mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.4011mL12.0057mL24.0113mL5mM0.4802mL2.4011mL4.8023mL10mM0.2401mL1.2006mL2.4011mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(protectfromlight)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?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(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:2.08mg/mL(4.99mM);Suspendedsolution;Needultrasonic2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(4.99mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.99mM);ClearsolutionBIOLOGICALACTIVITY?物活性EN4?種針對MYC的半胱氨酸171(C171)的共價配體。EN4對c-MYC的選擇性?于N-MYC和L-MYC。EN4抑制MYC轉(zhuǎn)錄活性，下調(diào)MYC靶標(biāo)，并具有抗腫瘤作?。體外研究EN4(1-50μM;for72hours)treatmentsignificantlyimpaires231MFPbreastcancercellproliferationinadosedependentmanner,with>90%inhibitionofproliferationat50μM[1].EN4(50μM;for60hours)treatmentsignificantlydecreasestheproteinlevelsofrepresentativeMYC-regulatedtargetgenes,includingCDK2andCDC25A.EN4treatmentalsosubstantiallyreducesMYClevels[1].EN4showsthestrongestinhibitionofbothMYC/MAXbindingtoitsDNAconsensussequenceinvitroaswellasMYCtranscriptionalactivityincells.EN4inhibitedMYC/MAXbindingtotheE-boxresponseelementDNAconsensussequenceinadose-responsivemannerwithanIC50valueof6.7μM.EN4alsoinhibitsMYCluciferasereporteractivityinadose-responsivemannerwithanIC50valueof2.8μM[1].EN4(50μM;for2hours)treatmentsignificantlyreducedMYCthermalstabilityin231MFPbreastcancercells[1].CellProliferationAssay[1]CellLine:231MFPbreastcancercellsConcentration:1μM,10μM,50μMIncubationTime:72hoursResult:Significantlyimpaired231MFPbreastcancercellproliferationinadose-dependentmanner.WesternBlotAnalysis[1]CellLine:231MFPbreastcancercellsConcentration:50μMIncubationTime:60hoursResult:TheproteinlevelsofCDK2andCDC25Aweresignificantlylowered.體內(nèi)研究EN4(50mg/kg;intraperitonealinjection;daily;for3weeks)treatmentsignificantlyattenuatedtumorgrowthin231MFPbreasttumorxenograftmice[1].AnimalModel:SCIDmiceinjectedwith231MFPbreastcancercells[1]2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEDosage:50mg/kgAdministration:Intraperitonealinjection;daily;for3weeksResult:Significantlyattenuatedtumorgrowthinvivo.REFERENCES[1].LydiaBoike,etal.DiscoveryofaFunctionalCovalentLigandTargetinganIntrinsicallyDisorderedCysteinewithinMYC.CellChemBiol.2021Jan21;28(1):4-13.e17.McePdfHeightCaution:Producthasnotbeenfully