Mdivi-1-Mitochondrial-division-inhibitor-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEMdivi-1Cat.No.:HY-15886CASNo.:338967-87-6Synonyms:Mitochondrialdivisioninhibitor1分⼦式:C₁₅H₁₀Cl₂N₂O₂S分⼦量:353.22作⽤靶点:Dynamin;Mitophagy;Autophagy;Apoptosis作⽤通路:Cytoskeleton;Autophagy;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:160mg/mL(452.98mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.8311mL14.1555mL28.3110mL5mM0.5662mL2.8311mL5.6622mL10mM0.2831mL1.4155mL2.8311mL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：0.5%CMC-Na/salinewater1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:2.5mg/mL(7.08mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥4mg/mL(11.32mM);Clearsolution3.请依序添加每种溶剂：17%Polyethyleneglycol12-hydroxystearateinsalineSolubility:10mg/mL(28.31mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Mdivi-1选择性的发动蛋⽩相关蛋⽩1(Drp1)抑制剂。Mdivi-1⼀种有效的线粒体分裂/线粒体⾃噬(mitophagy)抑制剂。体外研究Mdivi-1inhibitsDnm1GTPaseactivityinadose-dependentmanner,withanestimatedEC50of1-10μM.Mdivi-1increasestheapparentK0.5forGTP,lowerstheapparentVmaxforGTPhydrolysis,andcausesanincreaseintheHillcoefficientobservedforGTPintheDnm1GTPhydrolysisreaction[1].Cellstreatedwithmdivi-1displaydecreasedcytochromecreleaseandareducedrateofphosphatidylserineexposureontheirsurfacefollowingapoptosisinduction,consistentwithaninhibitionofapoptosisandwithpreviousstudiesusingotherstrategiestocompromiseDRP1activity[2].Mdivi-1resultsinapoptoticcelldeathinischemicretina[3].体内研究ThemitochondrialdivisionDRP,Dnm1,isthetargetofmdivi-1invivo.Mdivi-1quantitativelyblocksGMPPCP-dependentDnm1self-assemblyinaconcentrationrangesimilartoitseffectsonmitochondrialdivisioninvivo[1].Mdivi-1(50mg/kg,i.p.)significantlydecreasesGFAPproteinexpressioninthenormalmouseretina[3].PROTOCOLKinaseAssay[1]AllGTPaseassayreactionsarestartedina200μLvolume,ofwhich150μLisplacedintothewellofa96-wellplate.DepletionofNADH,asmonitoredbyreadingtheA340ofthereaction,ismeasuredevery20sforatotalof40minusingaSpectraMAX25096-wellplatereader.SpectrophotometricdataaretransferredtoExcelandthemeasuredsteadystatedepletionofNADHovertimeisconvertedtoproteinactivity.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.CellAssay[1]YPGlycerolplatesaretoppedwith10mLYPGlycerolcontaining1%lowmeltagarand75μMmdivi-1,andcellsarespotted12hourslaterusinga48wellpinningdevice.Afterpinningcells,platesareincubatedat24°Cor37°CandimagedusinganEagleEyeIIimagingsystem.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•CellMolImmunol.2022Jan;19(1):67-78.•NatCommun.2022Jul6;13(1):3882.•JHazardMater.15February2022,127268.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•Autophagy.2021Nov;17(11):3592-3606.•Autophagy.2020Aug;16(8):1413-1435.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].Cassidy-StoneA,etal.ChemicalinhibitionofthemitochondrialdivisiondynaminrevealsitsroleinBax/Bak-dependentmitochondrialoutermembranepermeabilization.DevCell.2008Feb;14(2):193-204.[2].TanakaA,etal.AchemicalinhibitorofDRP1uncouplesmitochondrialfissionandapoptosis.MolCell.2008Feb29;29(4):409-10.[3].ParkSW,etal.Aselectiveinhibitorofdrp1,mdivi-1,increasesretinalganglioncellsurvivalinacuteischemicmouseretina.InvestOphthalmolVisSci.2011Apr27;52(5):2837-43.Mce