Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEDIM-C-pPhOHCat.No.:HY-112055CASNo.:151358-47-3分?式:C??H??N?O分?量:338.4作?靶點(diǎn):Apoptosis作?通路:Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:125mg/mL(369.39mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.9551mL14.7754mL29.5508mL5mM0.5910mL2.9551mL5.9102mL10mM0.2955mL1.4775mL2.9551mL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。-80°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)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(shí)驗(yàn)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(shí)驗(yàn)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(6.15mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(6.15mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.15mM);ClearsolutionBIOLOGICALACTIVITY?物活性DIM-C-pPhOH核受體4A1(NR4A1)拮抗劑。DIM-C-pPhOH抑制癌細(xì)胞的?長和mTOR信號傳導(dǎo)，誘導(dǎo)細(xì)胞凋亡和細(xì)胞應(yīng)激。DIM-C-pPhOH可降低細(xì)胞增殖，對ACHN細(xì)胞和786-O細(xì)胞的IC50值分別為13.6μM和13.0μM。IC50&TargetNuclearreceptor4A1(NR4A1)[1]體外研究DIM-C-pPhOH(7.5-20μM;24hours;ACHNand786-Ocells)treatmentsignificantlydecreasescellproliferation[1].DIM-C-pPhOH(20μM;24hours;ACHNand786-Ocells)treatmentinducesAnnexinVstaininginACHNand786-Ocells,confirmingthatDIM-C-pPhOHinduceapoptosis,andalsoinducescleavageofcaspases7and8[1].DIM-C-pPhOH(15-20μM;24hours;ACHNand786-Ocells)treatmentinhibitsNR4A1-regulatedexpressionofsurvivin,bcl-2andEGFRinACHNand786-Ocells.Andalsoinducessestrin2,activatesAMPKαandinhibitsactivationofmTORanddownstreamkinases[1].DIM-C-pPhOHdecreasesexpressionofβ1-integrinproteinandmRNAandβ1-integrin-dependentresponsesinMCF7,MDA-MB-231,andSKBR3cellsandalsoinhibitsmigrationofthelattertwocelllines[2].CellProliferationAssay[1]CellLine:ACHNand786-OcellsConcentration:7.5μM,15μM,20μMIncubationTime:24hoursResult:Significantlydecreasedcellproliferation.ApoptosisAnalysis[1]CellLine:ACHNand786-OcellsConcentration:20μMIncubationTime:24hoursResult:InducedapoptosisinACHNand786-Ocells.WesternBlotAnalysis[1]2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECellLine:ACHNand786-OcellsConcentration:15μM,20μMIncubationTime:24hoursResult:InhibitedNR4A1-regulatedexpressionofsurvivin,bcl-2andEGFRinACHNand786-Ocells.Andalsoinducedsestrin2,activatedAMPKαandinhibitedactivationofmTORanddownstreamkinases.體內(nèi)研究DIM-C-pPhOH(30mg/kg;oralgavage;daily;for50days;maleathymicnudemice)treatmentresultsinasignificantinhibitionoftumorgrowth[1].AnimalModel:Maleathymicnudemice(aged6-7weeks)injectedwithACHNcells[1]Dosage:30mg/kg/dayAdministration:Oralgavage;daily;for50daysResult:Resultedinasignificantinhibitionoftumorgrowth.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?RedoxBiol.2021Jan;38:101807.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].HedrickE,etal.NuclearReceptor4A1(NR4A1)asaDrugTargetforRenalCellAdenocarcinoma.PLoSOne.2015Jun2;10(6):e0128308.[2].HedrickE,etal.NR4A1AntagonistsInhibitβ1-Integrin-DependentBreastCancerCellMigration.MolCellBiol.2016Apr15;36(9):1383-94.McePdfHeightCaution:Producth