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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/Z-VAD-FMK（同义词：Z-VAD（OMe）-FMK；Z-Val-Ala-Asp（OMe）-FMK）/HY-16658/1mg
商品详细Medchemexpress/Z-VAD-FMK（同义词：Z-VAD（OMe）-FMK；Z-Val-Ala-Asp（OMe）-FMK）/HY-16658/1mg
Medchemexpress/Z-VAD-FMK（同义词：Z-VAD（OMe）-FMK；Z-Val-Ala-Asp（OMe）-FMK）/HY-16658/1mg
Medchemexpress/Z-VAD-FMK（同义词：Z-VAD（OMe）-FMK；Z-Val-Ala-Asp（OMe）-FMK）/HY-16658/1mg
商品编号： HY-16658-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥3700.00
美元价： 2220.00
产地： 美国(厂家直采)
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产品分类： 小分子
公司分类： Small_molecule
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商品介绍
Z-VAD-FMKisacell-permeable,pan-caspaseinhibitor.

CustomerValidation

  • •CancerLett.2017Feb16;393:22-32.
  • •CancerLett.2016Aug28;379(1):134-142.
  • •AnalChem.2017Sep19;89(18):9788-9796.
  • •EnvironSciTechnol.2017Dec5;51(23):13938-13948.
  • •CellDeathDis.2017May25;8(5):e2810.
  • •BrJPharmacol.2017Sep;174(17):2941-2961.
  • •MolOncol.2017Aug;11(8):1035-1049.
  • •Oncotarget.2017May9;8(19):31297-31304.
  • •Oncotarget.2016Dec20;7(51):84810-84825.
  • •SciRep.2017Nov23;7(1):16111.
  • •SciRep.2017Oct19;7(1):13571.
  • •SciRep.2017Jun7;7(1):2929.
  • •SciRep.2016Dec1;6:38267.
  • •ToxicolApplPharmacol.2016Feb1;292:56-64.
  • •CancerMed.2017Feb;6(2):471-482.
  • •JEthnopharmacol.2017Aug12;212:8-17.
  • •BiomedPharmacother.2017Apr5;90:446-454.
  • •OncolRep.2017Feb;37(2):1270-1276.
  • •BiochemBiophysResCommun.2016Mar18;471(4):539-44.
  • •ChineseJournalofCellBIOLOGy.2016,38(10):1232-1243.
Description

Z-VAD-FMKisacell-permeable,pan-caspaseinhibitor.

IC50&Target

pan-caspase[1]

InVitro

Z-VAD-FMKisabroad-spectrumcaspaseinhibitor,hasbeenshowntoinhibittheintracellularactivationofcaspase-likeproteases.TheinjectionofZ-VAD-FMKsuppressesthecaspase-3activityinlungtissues,andsignificantlydecreasesthenumberofterminaldUTPnick-endlabeling-positivecells[1].Z-VAD-FMKisadmiNISTeredintraperitoneallyat1hourbeforeand6hoursafterSAH.Expressionofcaspase-3andpositiveTUNELisexaminedasMarkersforapoptosis.Z-VAD-FMKsuppressesTUNELandcaspase-3staininginendothelialcells,decreasescaspase-3activation,reducesBBBpermeABIlity,relievesvasospasm,abolishesbrainedema,andimprovesneurologicaloutcome[2].Z-VAD-FMKisacell-permeablecaspaseinhibitor,efficientlyblockscelldeathinducedbySMNdeficiency[3].

InVivo

ThesurvivalrateofmiceisprolongedsignificantlybytheinjectionofZ-VAD-FMK.AllmicesuccumbedtoLPSwithin30hours.Bycontrast,themicetreatedwithZ-VAD-FMKsurvivesignificantlylongerand27%ofthemicesurvivedmorethan7days[1].

References

  • [1].KawasakiM,etal.Protectionfromlethalapoptosisinlipopolysaccharide-inducedacutelunginjuryinmicebyacaspaseinhibitor.AmJPathol.2000Aug;157(2):597-603.

    [2].ParkS,etal.Neurovascularprotectionreducesearlybraininjuryaftersubarachnoidhemorrhage.Stroke.2004Oct;35(10):2412-7.

    [3].IlangovanR,etal.InhibitionofapoptosisbyZ-VAD-fmkinSMN-depletedS2cells.JBiolChem.2003Aug15;278(33):30993-9.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.1391mL10.6954mL21.3908mL
5mM0.4278mL2.1391mL4.2782mL
10mM0.2139mL1.0695mL2.1391mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[3]

Z-VAD-FMKisdissolvedinDMSOandstored,andthendilutedwithappropriatemediumbeforeuse[3].

PCRproductscontainingcodingsequencesforthedSMN(forwardprimer:5′-TAATACGACTCACTATAGGGAAGACGTACGACGAGTCG-3′;andreverseprimer:5′-TAATACGACTCACTATAGGGGTGGTGCTGGCTTCTTTC-3′;productlength,601bps;boldanditalicslettersrepresentT7promotersequences)andcontrolDrosophilaPresenilin(dPsn)gene(forwardprimer:5′-TAATACGACTCACTATAGGGTGGCTGCTGTCAATCTC-3′;andreverseprimer:5′-TAATACGACTCACTATAGGGCGATAGCAACGCTTCTTG-3′;productlength:543bps)areobtainedandgel-purified.Double-strandedRNAs(dsRNA)aregeneratedbytranscriptionwithRibomaxT7TranscriptionkitanddigestedwithRnase-freeDNase.ThedsRNAproductsareethanolprecipitatedandannealedbyincubationat65°Cfor30minandthenslowlyallowedtocoolatroomtemperature.TheannealeddsRNAproductsareanalyzedona1%agaorsegeltoensurethemajorityofdsRNAexistedasasingleband.ThedsRNA(2μg)and/orplasmidDNAs(2μg)areintroducedintocellsbyusingCellfectin.Caspaseinhibitionisachievedbyusing50μMofZ-VAD-FMKintheculturemedium[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdministration
[1][2]

Z-VAD-FMKisdissolvedat2mg/mLin1%DMSOinsterilesaline(Mice)[1].
Z-VAD-FMKisdissolvedin1%DMSOandfurtherdilutedinphysiologicalbuffersolution(final<0.01% dmso)="">[2].

Mice[1]
Miceusedinthisstudyare5-to6-week-old(20to22g)ICRmales.Miceareinjectedwith30mg/kgLPSfromE.coliSEROtypeO111:B4throughthetailvein.AsingleintravenousinjectionofZ-VAD.fmk(0.25mg)ismade15minutesbeforeLPSinjection,followedbythreeintravenousinjectionsofZ-VAD-FMK(0.1mgeach)perhour.Controlmiceareinjectedwiththesamevolumeof1%DMSOinsterilesaline.
Rat[2]
MaleSprague-Dawleyratsweighing300to350gareanesthetizedwithα-chloralose(40mg/kgIP)andurethane(400mg/kgIP).Animalsareintubated,andrespirationismaintainedwithasmallanimalrespirator.Rectaltemperatureismaintainedat37±0.5°Cwithaheatingpad.Theleftexternalcarotidarteryisisolatedanda4.0monofilamentnylonsutureisinsertedthroughtheinternalcarotidarterytoperforatethemiddlecerebralartery.SAHisconfirmedatautopsyineachrat.Sham-operatedratsunderwentthesameproceduresexceptthatthesutureiswithdrawnafterresistanceisfelt.Z-VAD-FMK(50μMper0.3mL)isinjectedintraperitoneallyat1hourbeforeand6hoursafterSAHinduction.Invehiclegroup,ratsunderwentSAHinductionandaretreatedwiththesamevolumeofvehicle(DMSOdilutedinphysiologicalbuffersolution).Notreatmentisappliedinsham-operatedanimals.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].KawasakiM,etal.Protectionfromlethalapoptosisinlipopolysaccharide-inducedacutelunginjuryinmicebyacaspaseinhibitor.AmJPathol.2000Aug;157(2):597-603.

    [2].ParkS,etal.Neurovascularprotectionreducesearlybraininjuryaftersubarachnoidhemorrhage.Stroke.2004Oct;35(10):2412-7.

    [3].IlangovanR,etal.InhibitionofapoptosisbyZ-VAD-fmkinSMN-depletedS2cells.JBiolChem.2003Aug15;278(33):30993-9.

MolecularWeight

467.49

Formula

C₂₂H₃₀FN₃O₇

CASNo.

187389-52-2

Storage
Powder-80°C2years
 -20°C1year
Insolvent-80°C6months
 -20°C1month
Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥30mg/mL

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

Purity:>98.0%