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Medchemexpress/Dynasore/HY-15304/10mg
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Medchemexpress/Dynasore/HY-15304/10mg
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DynasoreisaninhibitoroftheGTPaseactivityofdynaminwithanIC50of15μM.
Description

DynasoreisaninhibitoroftheGTPaseactivityofdynaminwithanIC50of15μM.

IC50&Target

IC50:15μM(GTPaseactivityofdynamin1and2)[1]

InVitro

DynasoreinterfereswiththeGTPaseactivityofdynamin1,dynamin2,andDrp1,themitochondrialdynamin,butnotofothersmallGTPases.Dynasoreactsasapotentinhibitorofendocyticpathwaysknowntodependondynaminbyrapidlyblockingcoatedvesicleformationwithinsecondsofdynasoreaddition.Twotypesofcoatedpitintermediatesaccumulateduringdynasoretreatment,g-shaped,halfformedpitsandO-shaped,fullyformedpits,capturedwhilepinchingoff[1].DynasoreinhibitsHSV-1andHSV-2infectionofhumanepithelialandneuronalcells,includingprimarygenitaltractcellsandhumanfetalneuronsandastrocytes.Dynasorereducesthenumberofviralcapsidsreachingthenuclearporeifaddedatthetimeofviralentryandthat,whenaddedaslateas8hpostentry,dynasoreblocksthetransportofnewlysynthesizedviralproteinsfromthenucleustothecytosol[2].Dynasorepreventsischemia/reperfusioninducedelevationofleftventricularenddiastolicpressure.DynasorealsodecreasescardiactroponinIeffluxduringreperfusionandreducesinfarctsize.Inculturedadultmousecardiomyocytessubjectedtooxidativestress,dynasoreincreasescardiomyocytesurvivalandviABIlity[3].

InVivo

Dynasoreamelioratesthemotordysfunctiongreatlyat3,7,and10daysafterSCIinrats.DynasoresignificantlyenhancesmotorfunctionwhichmaybebyinhibitingtheactivationofneuronalmitochondrialapoptoticpathwayandastrocyticproliferationinratsafterSCI[4].

References
  • [1].MaciaE,etal.Dynasore,acell-permeableinhibitorofdynamin.DevCell.2006Jun;10(6):839-50.

    [2].MuesMB,etal.Dynasoredisruptstraffickingofherpessimplexvirusproteins.JVirol.2015Jul;89(13):6673-84.

    [3].GaoD,etal.DynasoreprotectsmitochondriaandimprovescardiaclusitropyinLangendorffperfusedmouseheart.PLoSOne.2013Apr15;8(4):e60967.

    [4].LiG,etal.DynasoreImprovesMotorFunctionRecoveryviaInhibitionofNeuronalApoptosisandAstrocyticProliferationafterSpinalCordInjuryinRats.MolNeurobiol.2016Nov7.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM3.1026mL15.5130mL31.0260mL
5mM0.6205mL3.1026mL6.2052mL
10mM0.3103mL1.5513mL3.1026mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[3]

MouseventricularmyocytesareisolatedfrommaleadultC6/Blackmouse.Cardiomyocytessubjectsto2hoursofdrugtreatmentfollowedbyoxidativestress(30µMH2O2for35min).ForATPsupplementexperiments,thecellsaretreatedwith3mMATPfor30minbeforeexposuretoH2O2.Cardiomyocytesurvivalandviabilityareanalyzedbytrypanblueexclusion(TBE)assay[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdmiNISTration
[4]

Rat:Inthedynasoregroups,theratsaregivendynasoreimmediatelyatadoseof1,10,or30mg/kgthroughintraperitonealinjectionafterSCI,whiletheratsintheshamandSCIgroupsreceiveDMSO(samevolumeasdynasoregroups)throughintraperitonealinjection[4].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References
  • [1].MaciaE,etal.Dynasore,acell-permeableinhibitorofdynamin.DevCell.2006Jun;10(6):839-50.

    [2].MuesMB,etal.Dynasoredisruptstraffickingofherpessimplexvirusproteins.JVirol.2015Jul;89(13):6673-84.

    [3].GaoD,etal.DynasoreprotectsmitochondriaandimprovescardiaclusitropyinLangendorffperfusedmouseheart.PLoSOne.2013Apr15;8(4):e60967.

    [4].LiG,etal.DynasoreImprovesMotorFunctionRecoveryviaInhibitionofNeuronalApoptosisandAstrocyticProliferationafterSpinalCordInjuryinRats.MolNeurobiol.2016Nov7.

MolecularWeight

322.31

Formula

C₁₈H₁₄N₂O₄

CASNo.

304448-55-3

Storage
Powder-20°C3years
 4°C2years
Insolvent-80°C6months
 -20°C1month
Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

10mMinDMSO

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

Purity:99.61%