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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/LY294002(Synonyms: NSC 697286; SF 1101)/HY-10108/100mg
商品详细Medchemexpress/LY294002(Synonyms: NSC 697286; SF 1101)/HY-10108/100mg
Medchemexpress/LY294002(Synonyms: NSC 697286; SF 1101)/HY-10108/100mg
Medchemexpress/LY294002(Synonyms: NSC 697286; SF 1101)/HY-10108/100mg
商品编号： HY-10108-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥1320.00
美元价： 792.00
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
LY294002isabroad-spectruminhibitorofPI3K,withIC50of0.5/0.57/0.97μMforPI3Kα/δ/β,respectively,alsopotentlyinhibitsCK2withIC50of98nM.

CustomerValidation

  • •JExpMed.2016Dec12;213(13):2989-3005.
  • •DevCell.2016Oct24;39(2):239-253.
  • •CellMolLifeSci.2017Oct25.
  • •CellPhysiolBiochem.2016;40:579-588.
  • •EnvironPollut.2017Oct;229:964-975.
  • •JMolMed(Berl).2017Nov3.
  • •IntJBiolSci.2016Mar30;12(5):607-16.
  • •JTraumaAcuteCareSurg.2017Oct;83(4):683-689.
  • •ExpGerontol.2017Oct25;100:77-86.
  • •IntJOncol.2016Jul;49(1):422-30.
  • •BrainResBull.2017Aug24;134:236-245.
  • •JCancer.2016Jun5;7(9):1114-24.
  • •BiomedPharmacother.2017Jun15;93:130-145.
  • •BiochemBiophysResCommun.2017Aug26;490(3):1059-1065.
  • •BiomedicalResearch2017;28(8):3383-3386
  • •BosnJBasicMedSci.2017May20;17(2):132-137.
  • •LingnanModernClinicsinSurgery.Jun.2014,Vol.14No.3.
Description

LY294002isabroad-spectruminhibitorofPI3K,withIC50of0.5/0.57/0.97μMforPI3Kα/δ/β,respectively,alsopotentlyinhibitsCK2withIC50of98nM.

IC50&Target

IC50:0.5/0.57/0.97μM(PI3Kα/δ/β)[1]
IC50:98nM(CK2)[2]

InVitro

LY294002(5μM)completelyinhibitsthephosphorylationofPKBInHepG2cells.LY294002(5μM)isalsoshowntoblockinsulin-inducedphosphorylationofPKBSer473inCHO-IRcells[1].LY294002isalsoapotentinhibitorofCK2(caseinkinase2)withIC50of98nM.LY294002isalsoabletoreducethekinaseactivityofbothisoformsoftheserine/threoninekinasesGSK3αandβ[2].WhentheCNE-2ZcelllineisculturedinmediumcontainingLY294002(0μM,10μM,25μM,50μM,and75μM)for24hand48h,cellproliferationisremarkablydecreasedinadose-dependentfashion[3].

InVivo

TreatmentwithLY294002(i.p.,50mg/kg,75mg/kg)significantlyreducesmeanNPCtumorburdenascomparedwiththecontrolgroup.Treatmentwith10mg/kgor25mg/kgLY294002islesseffectiveindecreasingtumorburden.MeanNPCtumorburdentreatedwithLY294002isremarkablydecreasedinadose-dependentmanner,whereasmeanbodyweightisnoobviousdifferencebetweencontrolandtreatedgroups(LY294002,10mg/kg,25mg/kg,50mg/kg,and75mg/kg)[3].

References

  • [1].ChaussadeC,etal.EvidenceforfunctionalredundancyofclassIAPI3Kisoformsininsulinsignalling.BiochemJ.2007Jun15;404(3):449-58.

    [2].GharbiSI,etal.ExploringthespecificityofthePI3KfamilyinhibitorLY294002.BiochemJ.2007May15;404(1):15-21.

    [3].JiangH,etal.Phosphatidylinositol3-kinaseinhibitor(LY294002)inducesapoptosisofhumannasopharyngealcarcinomainvitroandinvivo.JExpClinCancerRes.2010Apr22;29:34.

    [4].UedaK,etal.DifferentialeffectsofLY294002andwortmanninonneuronsandvascularendothelialcellsintheratretina.PharmacolRep.2013;65(4):854-62.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM3.2537mL16.2686mL32.5373mL
5mM0.6507mL3.2537mL6.5075mL
10mM0.3254mL1.6269mL3.2537mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
KinaseAssay
[2]

PI3KinhibitionbyPI828andLY294002isdeterminedinarADIometricassayusingpurified,recombinantenzymes(classIAandclassIB)with1μMATP.Thekinasereactioniscarriedoutfor1hatroomtemperature(24°C)andisterminatedbyadditionofPBS.IC50valuesaresubsequentlydeterminedusingasigmoidaldose-responsecurvefit(variableslope).CK2andGSK3β(glycogensynthasekinase3β)inhibitionisestablishedbykinaseselectivityscreening.Inhibitor(10μM;PI828andLY294002)istestedagainsttheUpstatepanelofkinasesin10μMATP[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

CellAssay
[3]

LY294002isdissolvedinDMSOandstored,andthendilutedwithappropriatemedia(DMSO0.5%)beforeuse[3].

HumannasopharyngealcarcinomacelllineCNE-2Zisseededinto96-wellplatesat5000cells/well.Twenty-fourhoursaftercellsareseeded,themediumisremovedandreplacedinthepresenceofLY294002(0μM,10μM,25μM,50μM,and75μM)dissolvedinDMSOorDMSOonlyforanadditional24hand48h.ToavoidanynonspecifictoxiceffectsofDMSOoncellgrowth,DMSOconcentrationsaremaintainedat0.5%inallexperiments.MTTdye(5mg/mL)isaddedtoeachwell.ThereactionisstoppedbytheadditionofDMSO,andopticaldensityismeasuredat490nmonamultiwellplatereader.Backgroundabsorbanceofthemediumintheabsenceofcellsissubtracted.Allsamplesareassayedintriplicate,andthemeanforeachexperimentiscalculated.Resultsareexpressedasapercentageofcontrol,whichisconsideredtobe100%[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdmiNISTration
[3][4]

LY294002isdissolvedinvehicle(DMSO).

Mice[3]
Athymicnudemiceareusedwhentheyare6-8weeks.Micearerandomlydividedintofreeseparatedintofivegroups(n=4mice).Micearehousedinthesameenvironmentwithcontrolledtemperature,humidity,anda12hlight/darkcycle.MiceareinoculatedsubcutaneouslywithCNE-2Zcells(1×106cells/mousein200μLofRPMI-1640)intotheflank.Thetumortakerateis100%.After1week,anintraperitonealinjectionisperformedtothexenograftmicewithdifferentdosageofLY294002(10mg/kg,25mg/kg,50mg/kg,and75mg/kgtwiceweekly(n=4mice),eachgroupfor4weeks.Treatedmicearemonitoredanysigns.Bodyweightandtumorssizearemeasuredtwiceaweek.Tumorsizeismeasuredusingcalipersandtumorvolumeiscalculated(volume=longaxis×shortaxis2).Attheendofthetreatment,allmiceareeuthanized.Onepartoftumortissueisfixedinformalinandembeddedinparaffin,andanotherpartisstoredat-70°C.
Rat[4]
MaleSprague-Dawleyratsweighing220-240gareanesthetizedbyintraperitoneallyinjectingpentobarbitalsodium(50mg/kg).Theanimalsaredividedinto3groups:NMDA+vehicle(DMSO)(n=46),NMDA+LY294002(50nmol)(n=25),andNMDA+Wortmannin(50nmol)(n=23).EitherLY294002orwortmanninmixedwith200nmolofNMDAinatotalvolumeof5μLisinjectedintothevitreouscavityofoneeye.ThesamevolumeofDMSOisinjectedintothevitreouscavityofthecontralateraleye,whichisusedasacontrol.Theinjectionsareperformedunderamicroscopeusinga32-gaugeneedle,whichisconnectedtoamicrosyringe.Theneedleisinsertedapproximately1mmbehindthecorneallimbus.Damagetoneuronsandbloodvesselsintheretinaisassessedat2and7daysaftertheinjection.TheeffectsoftheintravitrealtreatmentwitheitherLY294002orWortmanninaloneonretinalneuronsandbloodvesselsarealsoexamined.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].ChaussadeC,etal.EvidenceforfunctionalredundancyofclassIAPI3Kisoformsininsulinsignalling.BiochemJ.2007Jun15;404(3):449-58.

    [2].GharbiSI,etal.ExploringthespecificityofthePI3KfamilyinhibitorLY294002.BiochemJ.2007May15;404(1):15-21.

    [3].JiangH,etal.Phosphatidylinositol3-kinaseinhibitor(LY294002)inducesapoptosisofhumannasopharyngealcarcinomainvitroandinvivo.JExpClinCancerRes.2010Apr22;29:34.

    [4].UedaK,etal.DifferentialeffectsofLY294002andwortmanninonneuronsandvascularendothelialcellsintheratretina.PharmacolRep.2013;65(4):854-62.

MolecularWeight

307.34

Formula

C₁₉H₁₇NO₃

CASNo.

154447-36-6

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:14.9mg/mL

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

Purity:99.97%