LY294002-hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemELY294002hydrochlorideCat.No.:HY-10108ACASNo.:934389-88-5分?式:C??H??ClNO?分?量:343.8作?靶點(diǎn):PI3K;CaseinKinase;DNA-PK;Apoptosis作?通路:PI3K/Akt/mTOR;CellCycle/DNADamage;StemCell/Wnt;Apoptosis儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性L(fǎng)Y294002hydrochloride?種有效的?譜PI3K抑制劑，對(duì)P110α,P110δ和P110β的IC50分別為0.5,0.57和0.97μM。IC50值分別為P110α、P110δ和P110β的0.5、0.57和0.97μM。LY294002hydrochloride也能抑制CK2，其IC50為98nM。LY294002hydrochloride可?于胰腺癌研究[1][2][3]。IC50&TargetCK2CK2α20.098μM(IC50)3.869μM(IC50)體外研究LY294002hydrochloride(0-75μM;24hoursand48hours)remarkablydecreaseshumannasopharyngealcarcinomaCNE-2Zcellsinadose-dependentfashion[4].LY294002hydrochloride(0-75μM;24hoursand48hours)inducesCNE-2Zcellsapoptosisrateindose-dependent[4].LY294002hydrochloride(10-75μM)significantlydecreasesp-Akt(S473)expressionlevelsandup-regulatescaspase-9activityinCNE-2Zcells.TotalAktproteinlevelisnotdifferencewithdifferentconcentration[4].LY294002hydrochloride(5,10,100μM;for2hours)treatmentpartiallysuppressesLysophosphatidicacid(LPA)-induced(20μM;for4hours)nucleartranslocationofYAP,accompaniedbyareductioninp-AKTlevels[6].CellProliferationAssayCellLine:CNE-2Zcells[4]Concentration:0μM,10μM,25μM,50μM,and75μM1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEIncubationTime:24hoursand48hoursResult:DecreasedCNE-2Zcellsinadose-dependentfashion.ApoptosisAnalysisCellLine:CNE-2Zcells[4]Concentration:0μM,10μM,25μM,50μM,and75μMIncubationTime:24hoursand48hoursResult:Inducedapoptosisrateinadose-dependentmanner.WesternBlotAnalysisCellLine:CNE-2Zcells[4]Concentration:0μM,10μM,25μM,50μM,and75μMIncubationTime:24hoursand48hoursResult:DecreasedphosphorylatedAkt(S473)expressionlevelsweresignificantly,up-regulatedcaspase-9activityinCNE-2Zcellsintreatedgroup.體內(nèi)研究LY294002hydrochloride(10,25,50,75mg/kg;i.p.;twiceweekly;for4weeks)significantlyreducesmeanNPCtumorburdeninadose-dependentmanner.LY294002(10,25mg/kg)islesseffectiveindecreasingtumorburden[4].LY294002hydrochloride(1.2mg/kgperday;i.p.;for14days)preventsLeptin(60ug/kg)-inducedadverseeffectsonspermatozoainSprague-Dawleyrats[5].AnimalModel:Athymicnudemice(6-8weeks)withCNE-2Zxenograft[4]Dosage:10mg/kg,25mg/kg,50mg/kg,and75mg/kgAdministration:IP;twiceweekly,for4weeksResult:MeanNasopharyngealcarcinoma(NPC)tumorburdenwasremarkablydecreasedinadose-dependentmanner.戶(hù)使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?MolCancer.2022May10;21(1):112.?SignalTransductTargetTher.2022Aug31;7(1):290.?SignalTransductTargetTher.2021Jun18;6(1):234.?Blood.2018Jul12;132(2):210-222.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE?CellMolImmunol.2020Mar;17(3):261-271.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].BaiR,etal.TheeffectofPI3KinhibitorLY294002andgemcitabinehydrochloridecombinedwithionizingradiationontheformationofvasculogenicmimicryofPanc-1cellsinvitroandinvivo.Neoplasma.2016;63(1):80-92.[2].ChaussadeC,etal.EvidenceforfunctionalredundancyofclassIAPI3Kisoformsininsulinsignalling.BiochemJ.2007Jun15;404(3):449-58.[3].GharbiSI,etal.ExploringthespecificityofthePI3KfamilyinhibitorLY294002.BiochemJ.2007May15;404(1):15-21.[4].JiangH,etal.Phosphatidylinositol3-kinaseinhibitor(LY294002)inducesapoptosisofhumannasopharyngealcarcinomainvitroandinvivo.JExpClinCancerRes.2010Apr22;29:34.[5].MdMokhtarAH,etal.LY294002,aPI3Kpathwayinhibitor,preventsleptin-inducedadverseeffectsonspermatozoainSprague-Dawleyrats.Andrologia.2019Apr;51(3):e13196.[6].Yi-JenHsueh,etal.LysophosphatidicacidinducesYAP-promotedproliferationofhumancornealendothelialcellsviaPI3KandROCKpathways.MolTherMethodsClinDev.2015Apr29;2:15014.Mc