MHY1485-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEMHY1485Cat.No.:HY-B0795CASNo.:326914-06-1分⼦式:C₁₇H₂₁N₇O₄分⼦量:387.39作⽤靶点:mTOR;Autophagy作⽤通路:PI3K/Akt/mTOR;Autophagy储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:7.69mg/mL(19.85mM;Needultrasonic)H2O:<0.1mg/mL(ultrasonic)(insoluble)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.5814mL12.9069mL25.8138mL5mM0.5163mL2.5814mL5.1628mL10mM0.2581mL1.2907mL2.5814mL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:≥0.77mg/mL(1.99mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥0.77mg/mL(1.99mM);Clearsolution3.请依序添加每种溶剂：20%HP-β-CDinsalineSolubility:1mg/mL(2.58mM);Suspendedsolution;Needultrasonic4.请依序添加每种溶剂：50%PEG300>>50%salineSolubility:5mg/mL(12.91mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性MHY1485⼀种有效的细胞渗透性mTOR激活剂，靶向mTOR的ATP结构域。MHY1485通过抑制⾃噬体和溶酶体之间的融合来抑制⾃噬(autophagy)。IC50&TargetmTORC1mTORC2Autophagy体外研究MHY1485(10μM;4hours)showsthatGCDC-inducedautophagicactivityisinhibitedbyupregulatingp-mTORexpressionanddownregulatingLC3andp62expressioninHCCcells[1].MHY1485(5μM;6hours)increasestheLC3II/LC3Iratioinadoseandtime-dependentlymannerduetopresumablyinhibitedLC3IIdegradationinratliverAc2Fcells[2].MHY1485(0.5-2μM;6hours)increasesthephosphorylationofmTORatser2448andupregulatesthelevelofphosphorylationof4E-BP1inadose-dependentlymannerinAc2Fcells[2].WesternBlotAnalysis[1]CellLine:HCCcellsConcentration:10μMIncubationTime:4hoursResult:Upregulatedp-mTORanddownregulatedLC3andp62expression.体内研究MHY1485(intraperitonealinjection;10ꢀmg/kg,2days)blockstheautophagysignalinginducedbyfollicle-stimulatinghormone(FSH).Itincreasesp-mTORandp-S6K1expressionlevels,whereasLC3expressionshowsnomarkedchangecomparedtothatinthecontrolgroup[3].AnimalModel:4-week-oldfemaleICRmice[3]Dosage:10ꢀmg/kg,2daysAdministration:IntraperitonealinjectionResult:SuppressedtheautophagylevelfollowingFSHtreatment.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE户使⽤本产品发表的科研⽂献•JInfect.2019Sep;79(3):262-276.•BoneRes.2022Jun22;10(1):45.•RedoxBiol.2022Aug4;55:102426.•CancerLett.2020Jan28;469:481-489.•CellDeathDis.2022Jun20;13(6):557.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].GaoL,etal.GlycochenodeoxycholatepromoteshepatocellularcarcinomainvasionandmigrationbyAMPK/mTORdependentautophagyactivation.CancerLett.2019Jul10;454:215-223.[2].ChoiYJ,etal.InhibitoryeffectofmTORactivatorMHY1485onautophagy:suppressionoflysosomalfusion.PLoSOne.2012;7(8):e43418.[3].ZhouJ,etal.Administrationoffollicle-stimulatinghormoneinducesautophagyviaupregulationofHIF-1αinmousegranulosacells.CellDeathDis.2017Aug17;8(8):e3001.McePdfHeightCaution:Producthasnotbee