Mdivi-1-Mitochondrial-division-inhibitor-1-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMdivi-1Cat.No.:HY-15886CASNo.:338967-87-6Synonyms:Mitochondrialdivisioninhibitor1分?式:C??H??Cl?N?O?S分?量:353.22作?靶點:Dynamin;Mitophagy;Autophagy;Apoptosis作?通路:Cytoskeleton;Autophagy;Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:160mg/mL(452.98mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.8311mL14.1555mL28.3110mL5mM0.5662mL2.8311mL5.6622mL10mM0.2831mL1.4155mL2.8311mL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，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?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：(為保證實驗結果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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：0.5%CMC-Na/salinewater1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:2.5mg/mL(7.08mM);Suspendedsolution;Needultrasonic2.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥4mg/mL(11.32mM);Clearsolution3.請依序添加每種溶劑：17%Polyethyleneglycol12-hydroxystearateinsalineSolubility:10mg/mL(28.31mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Mdivi-1選擇性的發(fā)動蛋?相關蛋?1(Drp1)抑制劑。Mdivi-1?種有效的線粒體分裂/線粒體?噬(mitophagy)抑制劑。體外研究Mdivi-1inhibitsDnm1GTPaseactivityinadose-dependentmanner,withanestimatedEC50of1-10μM.Mdivi-1increasestheapparentK0.5forGTP,lowerstheapparentVmaxforGTPhydrolysis,andcausesanincreaseintheHillcoefficientobservedforGTPintheDnm1GTPhydrolysisreaction[1].Cellstreatedwithmdivi-1displaydecreasedcytochromecreleaseandareducedrateofphosphatidylserineexposureontheirsurfacefollowingapoptosisinduction,consistentwithaninhibitionofapoptosisandwithpreviousstudiesusingotherstrategiestocompromiseDRP1activity[2].Mdivi-1resultsinapoptoticcelldeathinischemicretina[3].體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻?CellMolImmunol.2022Jan;19(1):67-78.?NatCommun.2022Jul6;13(1):3882.?JHazardMater.15February2022,127268.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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