AC-73-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAC-73Cat.No.:HY-122214CASNo.:775294-71-8分⼦式:C₂₁H₂₁NO₂分⼦量:319.4作⽤靶点:Autophagy作⽤通路:Autophagy储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥250mg/mL(782.72mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM3.1309mL15.6544mL31.3087mL5mM0.6262mL3.1309mL6.2617mL10mM0.3131mL1.5654mL3.1309mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(6.51mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(6.51mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.51mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性AC-73ClusterofDifferentiation147(CD147)的第⼀种特定的⼝服⽣物利⽤的抑制剂，可特异性破坏CD147的⼆聚化(结合位点在CD147的N端IgC2域中包括Glu64和Glu73)，从⽽抑制CD147/ERK1/2/STAT3/MMP-2途径，并抑制肝癌细胞的运动和侵袭。AC-73还⼀种抗增殖药，也⽩⾎病细胞⾃噬的诱导剂。IC50&TargetCD147[1]体外研究AC-73(5-10μM;24hours;SMMC-7721andHuh-7cells)treatmentsignificantlydecreasesthemigrationabilityofSMMC-7721andHuh-7cellsinadose-dependentmanneranddecreasestheinvasionoftwoHCCcellsinadose-dependentmannerat24hours.AC-73treatmentreducesHCCmetastases.TherearenoobviouseffectsoncellviabilitywhentwoHCCcellsaretreatedwithAC-73atamaximumconcentrationof20μM.ThepossiblebindingsitesofAC-73onCD147includedGlu64andGlu73intheN-terminalIgC2domain,whichtworesiduesarelocatedinthedimerinterfaceofCD147[1].AC-73(5-10μM;24hours;SMMC-7721cells)treatmentcouldsignificantlyinhibitbothMMP-2andMMP-9mRNAexpressionattheconcentrationof10μM,especiallyMMP-2,butnoobviouseffectonMMP-1,MMP-3,MMP-7,MMP-11norMMP-13.AC-73coulddosedependentlyreducetheexpressionofMMP-2mRNAlevelandsecretionoftheproteinlevelusingRT-qPCRanalysisandgelatinzymographyexperiments[1].AC-73(5-20μM;6hours;SMMC-7721cells)treatmentdose-dependentlysuppressesthephosphorylationofERK1/2andSTAT3[1].RT-PCR[1]CellLine:SMMC-7721cellsConcentration:5μMor10μMIncubationTime:24hoursResult:SignificantlyinhibitedbothMMP-2andMMP-9mRNAexpressionattheconcentrationof10μM.DosedependentlyreducedtheexpressionofMMP-2mRNAlevelandsecretionoftheproteinlevelusingRT-qPCRanalysisandgelatinzymographyexperiments.WesternBlotAnalysis[1]CellLine:SMMC-7721cellsConcentration:5μM,10μMor20μM2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEIncubationTime:6hoursResult:ThephosphorylationofERK1/2andSTAT3wasdose-dependentlysuppressed.体内研究AC-73(25-50mg/kg;for4weeks;MaleBALB/cnu/numice)treatmentsignificantlydecreasestheincidenceofmetastaticfociinnudemice.AC-73inhibitsthephosphorylationofERK1/2andSTAT3inadose-dependentmanner.MMP-2isalsoreducedbyAC-73.AC-73couldnotinhibittumorcellproliferationinvivo[1].AnimalModel:MaleBALB/cnu/numice(4-6weeks)withSMMC-7721cells[1]Dosage:25mg/kg,50mg/kgAdministration:Injected;daily;for3weeksResult:Significantlydecreasedtheincidenceofmetastaticfociinnudemice.InhibitedthephosphorylationofERK1/2andSTAT3inadose-dependentmanner.MMP-2wasalsoreduced.户使⽤本产品发表的科研⽂献•CancerLett.2021Aug30;S0304-3835(21)00428-6.•JCrohnsColitis.2022Jul14;jjac084.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].FuZG,etal.Anovelsmall-moleculecompoundtargetingCD147inhibitsthemotilityandinvasionofhepatocellularcarcinomacells.Oncotarget.2016Feb23;7(8):9429-47.[2].SpinelloI,etal.Thesmall-moleculecompoundAC-73targetingCD147inhibitsleukemiccellproliferation,inducesautophagyandincreasesthechemotherapeuticsensitivityofacutemyeloidleukemiacells.Haematologica.2019May;104(5):9