DIM-C-pPhOH-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEDIM-C-pPhOHCat.No.:HY-112055CASNo.:151358-47-3分⼦式:C₂₃H₁₈N₂O分⼦量:338.4作⽤靶点:Apoptosis作⽤通路:Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(369.39mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.9551mL14.7754mL29.5508mL5mM0.5910mL2.9551mL5.9102mL10mM0.2955mL1.4775mL2.9551mL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。-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。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(6.15mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(6.15mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.15mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性DIM-C-pPhOH核受体4A1(NR4A1)拮抗剂。DIM-C-pPhOH抑制癌细胞的⽣长和mTOR信号传导，诱导细胞凋亡和细胞应激。DIM-C-pPhOH可降低细胞增殖，对ACHN细胞和786-O细胞的IC50值分别为13.6μM和13.0μM。IC50&TargetNuclearreceptor4A1(NR4A1)[1]体外研究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—您⾝边的抑制剂⼤师www.MedChemECellLine:ACHNand786-OcellsConcentration:15μM,20μMIncubationTime:24hoursResult:InhibitedNR4A1-regulatedexpressionofsurvivin,bcl-2andEGFRinACHNand786-Ocells.Andalsoinducedsestrin2,activatedAMPKαandinhibitedactivationofmTORanddownstreamkinases.体内研究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.户使⽤本产品发表的科研⽂献•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