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Medchemexpress/DAPT(Synonyms: GSI-IX)/HY-13027/10mM*1mL in DMSO
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Medchemexpress/DAPT(Synonyms: GSI-IX)/HY-13027/10mM*1mL in DMSO
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MedChemExpress
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HY-13027-10mM*1mLinDMSO
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DAPTisaγ-secretaseinhibitor,reducesthetotalbeta-amyloidpeptide(Aβ)productionwithIC50of20nMinHEK293cells.

CustomerValidation

  • •Hepatology.2016Jul;64(1):175-88.
  • •JAllergyClinImmunol.2017Mar;139(3):987-996.e10.
  • •ProcNatlAcadSciUSA.2017May30;114(22):E4425-E4434.
  • •JCellPhysiol.2017Jul11.
  • •WorldJGastroenterol.2017Apr7;23(13):2330-2336.
  • •YaleUniversity.January2016
Description

DAPTisaγ-secretaseinhibitor,reducesthetotalbeta-amyloidpeptide(Aβ)productionwithIC50of20nMinHEK293cells.

IC50&Target

IC50:20nM(Aβ,inHEK293cells)[1]

InVitro

DAPTinhibitsAβproductionover90%,effectsonlyamodestreductioninAPPβintheculturemedia.AlthoughAPPβisreducedbyabout30%byDAPTtreatment,thiseffectisnotconcentration-dependentandisreversedbytheremovalofDAPT[1].CNE-2cellsaretreatedwithincreasingconcentrationsofDAPT(0,25,50and75μM),andtheγ-secretase-generatedNotch1fragmentVal1744-NICDisdecreasedafter48hinadose-dependentmanner(P<0.01). the="" activation="" of="" γ-secretase="" is="" almost="" completely="" inhibited="" by="" dapt="" at="" the="" concentration="" of="" 50="">[2].

InVivo

DAPTisadmiNISTeredtoPDAPPmice(100mg/kgs.c.)andthelevelsofDAPTandAβareexaminedinthebraincortex.PeakDAPTlevelsof490ng/gareachievedinthebrain3haftertreatment,andlevelsgreaterthan100ng/g(~200nM)aresustainedthroughoutthefirst18h.ThesebrainconcentrationsofDAPTareinexcessofitsIC50forloweringAβinneuronalcultures(115nM),andresultsinarobustandsustainspharmacodynamiceffect[1].DAPTprotectsbrainagainstcerebralischemiabydown-regulatingtheexpressionofNotch1andNuclearfactorkappaBinrats.WesternblotanalysesalsoshowasignificantdecreaseofNotch1andNF-κBexpressioninDAPT(0.03mg/kg)group(P<0.05 vs.="" mcao="">[3].

References

  • [1].DoveyHF,etal.Functionalgamma-secretaseinhibitorsreducebeta-amyloidpeptidelevelsinbrain.JNeuRochem.2001Jan;76(1):173-81.

    [2].ZhouJX,etal.γ-secretaseinhibitioncombinedwithcisplatinenhancesapoptosisofnasopharyngealcarcinomacells.ExpTherMed.2012Feb;3(2):357-361.

    [3].LiS,etal.DAPTprotectsbrainagainstcerebralischemiabydown-regulatingtheexpressionofNotch1andnuclearfactorκBinrats.NeurolSci.2012Dec;33(6):1257-64.

    [4].TanimizuN,etal.Intrahepaticbileductsaredevelopedthroughformationofhomogeneouscontinuousluminalnetworkanditsdynamicrearrangementinmice.Hepatology.2016Jul;64(1):175-88.

    [5].MichaelT.Chang,etal.NotchDrivesProliferationAndRADIationResistanceOfCancerStemCellsInAdenoidCysticCarcinoma.YaleUniversity.January2016.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.3124mL11.5618mL23.1235mL
5mM0.4625mL2.3124mL4.6247mL
10mM0.2312mL1.1562mL2.3124mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[1]

DAPTisdissolvedinDMSOandstored,andthendilutedwithappropriatemedia(DMSO0.1%)beforeuse[1].

Humanembryonickidneycells,transfectedwiththegeneforAPP751(HEK293)areusedforroutineAβreductionassays.Cellsareplatedin96-wellplatesandallowedtoadhereovernightinDulbecco"smodifiedEaglemedium(DMEM)supplementedwith10%heat-inactivatedfetalbovineserum.Cellsarepre-treatedfor2hat37°CwithDAPT(0,0.4,2,10,50and250nM),mediaareaspiratedoffandfreshcompoundsolutionsapplied.Afteranadditional2-htreatmentperiod,conditionedmediaaredrawnoffandanalyzedbyasandwichELISA(266-3D6)specificfortotalAβ.ReductionofAβproductionismeasuredrelativetocontrolcellstreatedwith0.1%DMSOandexpressedasapercentageinhibition.Datafromatleastsixdosesinduplicatearefittedtoafour-parameterlogisticalmodelusingXLfitsoftwareinordertodeterminepotency[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdministration
[1][3]

DAPTisformulatedincornoil,5%(v/v)ethanol(Mice)[1].
DAPTisdissolvedin0.01MPBSincluding5%DMSOtoprepareconcentrationsof8.3mg/mL(Rat)[3].

Mice[1]
Thethree-tofour-month-oldheterozygousPDAPPtransgenicmiceoverexpressingtheAPPV717Fmutantformoftheamyloidprecursorprotein.Eachtreatmentgroup(n=10)consistsofequalnumbersofage-matchedmaleandfemaleanimalsthatarefastedovernightpriortotreatment.Bothtreatmentandcontrolgroupsaredosedatavolumeof10mL/kgwithDAPTorvehiclealone.TissuesareprocessedandallAβandAPPmeasurementsaremade.Afterremovalofthebrain,thecortexfromonehemisphereishomogenized,extractedwith5Mguanidine,50mMTris-pH8.0,centrifuged,andthesupernatantisusedforAβmeasurements.Cortexfromtheotherhemisphereissnapfrozenforanalysisofcompoundlevels.Aβlevelsareexpressedasng/gofwettissueweight,andpercentagereductionsarecalculatedrelativetothemeanAβleveloftissuefromvehicle-treatedcontrolanimals.DataareanalyzedwithMann-Whitneynon-parametricstatisticstoassesssignificance.
Rat[3]
MaleSprague-Dawleyrats(260-290g)areused.DAPTsolutionisstereotacticallyinjectedintothelateralcerebralventricle(LV)immediatelyafterMCAO.ThestereotacticinjectionsintotheLVsareperformedatcoordinates−0.8mmanteroposterior,±1.5mmmediolateraland−4.5mmdorsoventralfromthebregma.30ratsarerandomlyassignedtothreeoperatinggroups(10ratsineachgroup):sham-operatedgroupthatreceiveequalvolumeofPBSwithoutMCAOoperation;MCAOgroupthatreceiveequalvolumePBSafterMCAO(MCAO);andDAPTgroupthatreceiveDAPTas0.03mg/kgafterMCAO.24hafteroperationthefirstneurologicalfunctionisassessedandthen48hafteroperationthesecondneurologicalfunctionisassessed.Meanwhile,brainwatercontentandinfarctionvolumearemeasuredandcomparedamongdifferentgroups.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].DoveyHF,etal.Functionalgamma-secretaseinhibitorsreducebeta-amyloidpeptidelevelsinbrain.JNeurochem.2001Jan;76(1):173-81.

    [2].ZhouJX,etal.γ-secretaseinhibitioncombinedwithcisplatinenhancesapoptosisofnasopharyngealcarcinomacells.ExpTherMed.2012Feb;3(2):357-361.

    [3].LiS,etal.DAPTprotectsbrainagainstcerebralischemiabydown-regulatingtheexpressionofNotch1andnuclearfactorκBinrats.NeurolSci.2012Dec;33(6):1257-64.

    [4].TanimizuN,etal.Intrahepaticbileductsaredevelopedthroughformationofhomogeneouscontinuousluminalnetworkanditsdynamicrearrangementinmice.Hepatology.2016Jul;64(1):175-88.

    [5].MichaelT.Chang,etal.NotchDrivesProliferationAndRadiationResistanceOfCancerStemCellsInAdenoidCysticCarcinoma.YaleUniversity.January2016.

MolecularWeight

432.46

Formula

C₂₃H₂₆F₂N₂O₄

CASNo.

208255-80-5

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥215mg/mL

DAPTismixedwitholiveoil[4].DAPTispreparedincornoil[5].

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

References

  • [1].DoveyHF,etal.Functionalgamma-secretaseinhibitorsreducebeta-amyloidpeptidelevelsinbrain.JNeurochem.2001Jan;76(1):173-81.

    [2].ZhouJX,etal.γ-secretaseinhibitioncombinedwithcisplatinenhancesapoptosisofnasopharyngealcarcinomacells.ExpTherMed.2012Feb;3(2):357-361.

    [3].LiS,etal.DAPTprotectsbrainagainstcerebralischemiabydown-regulatingtheexpressionofNotch1andnuclearfactorκBinrats.NeurolSci.2012Dec;33(6):1257-64.

    [4].TanimizuN,etal.Intrahepaticbileductsaredevelopedthroughformationofhomogeneouscontinuousluminalnetworkanditsdynamicrearrangementinmice.Hepatology.2016Jul;64(1):175-88.

    [5].MichaelT.Chang,etal.NotchDrivesProliferationAndRadiationResistanceOfCancerStemCellsInAdenoidCysticCarcinoma.YaleUniversity.January2016.

Purity:99.25%

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