LY294002-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemELY294002Cat.No.:HY-10108CASNo.:154447-36-6分⼦式:C₁₉H₁₇NO₃分⼦量:307.34作⽤靶点:PI3K;CaseinKinase;DNA-PK;Autophagy;Apoptosis作⽤通路:PI3K/Akt/mTOR;CellCycle/DNADamage;StemCell/Wnt;Autophagy;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months

-20°C1month溶解性数据体外实验DMSO:41.67mg/mL(135.58mM;Needultrasonic)扫描⼆维码，运⽤溶解⽅案计算器获得适合您实验体系的溶解⽅案MassSolvent1mg5mg10mgConcentration制备储备液1mM3.2537mL16.2686mL32.5373mL5mM0.6507mL3.2537mL6.5075mL10mM0.3254mL1.6269mL3.2537mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存⽅式和期限。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶1.请依序添加每种溶剂：10%DMSO40%PEG3005%Tween-8045%salineSolubility:≥2.25mg/mL(7.32mM);Clearsolution此⽅案可获得≥2.25mg/mL(7.32mM，饱和度未知)的澄溶液。以1mL⼯作液为例，取100μL22.5mg/mL的澄DMSO储备液加到400μLPEG300中，混合均匀；向上述1/4www.MedChemEwww.MedChemE2.体系中加⼊50μLTween-80，混合均匀；然后继续加⼊450μL⽣理盐⽔定容⾄1mL。请依序添加每种溶剂：10%DMSO90%(20%SBE-β-CDinsaline)Solubility:≥2.25mg/mL(7.32mM);Clearsolution此⽅案可获得≥2.25mg/mL(7.32mM，饱和度未知)的澄溶液。以1mL⼯作液为例，取100μL22.5mg/mL的澄DMSO储备液加到900μL20%的SBE-β-CD⽣理盐⽔⽔溶3.液中，混合均匀。请依序添加每种溶剂：10%DMSO90%cornoilSolubility:≥2.25mg/mL(7.32mM);Clearsolution此⽅案可获得≥2.25mg/mL(7.32mM，饱和度未知)的澄溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。4.以1mL⼯作液为例，取100μL22.5mg/mL的澄DMSO储备液加到900μL⽟⽶油中，混合均匀。请依序添加每种溶剂：5%DMSO95%(20%SBE-β-CDinsaline)Solubility:2.87mg/mL(9.34mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性LY294002⼀种⼴谱PI3K抑制剂，抑制PI3Kα,PI3Kδ和PI3Kβ的IC50分别为0.5,0.57,0.97μM。LY294002也可抑制CK2的活性，IC50为98nM。LY294002⼀种竞争性DNA-PK抑制剂，可逆结合DNA-PK的激酶结构域，IC50为1.4μM。LY294002⼀种⾃噬(autophagy)和凋亡(apoptosis)激活剂。IC50&Targetp110αp110δp110βhumanCK20.5μM(IC50)0.57μM(IC50)0.97μM(IC50)98nM(IC50)humanCK2α2DNA-PK3.869μM(IC50)1.4μM(IC50)体外研究LY294002(0-75μM;24hoursand48hours)remarkablydecreaseshumannasopharyngealcarcinomaCNE-2Zcellsinadose-dependentfashion[4].LY294002(0-75μM;24hoursand48hours)inducesCNE-2Zcellsapoptosisrateindose-dependent[4].LY294002(10-75μM)significantlydecreasesp-Akt(S473)expressionlevelsandup-regulatescaspase-9activityinCNE-2Zcells.TotalAktproteinlevelisnotdifferencewithdifferentconcentration[4].LY294002(5,10,100µM;for2hours)treatmentpartiallysuppressesLysophosphatidicacid(LPA)-induced(20µM;for4hours)nucleartranslocationofYAP,accompaniedbyareductioninp-AKTlevels[6].CellProliferationAssay[4]CellLine:CNE-2ZcellsConcentration:0μM,10μM,25μM,50μM,and75μMIncubationTime:24hoursand48hoursResult:DecreasedCNE-2Zcellsinadose-dependentfashion.ApoptosisAnalysis[4]2/4www.MedChemEwww.MedChemECellLine:CNE-2ZcellsConcentration:0μM,10μM,25μM,50μM,and75μMIncubationTime:24hoursand48hoursResult:Inducedapoptosisrateindose-dependent.WesternBlotAnalysis[4]CellLine:CNE-2ZcellsConcentration:10μM,25μM,50μM,and75μMIncubationTime:Result:DecreasedphosphorylatedAkt(S473)expressionlevelsweresignificantly,up-regulatedcaspase-9activityinCNE-2Zcellsintreatedgroup.体内研究LY294002(10,25,50,75mg/kg;i.p.;twiceweekly;for4weeks)significantlyreducesmeanNPCtumorburdeninadose-dependentmanner.LY294002(10,25mg/kg)islesseffectiveindecreasingtumorburden[4].LY294002(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:Intraperitonealinjection;twiceweekly,for4weeksResult:MeanNasopharyngealcarcinoma(NPC)tumorburdenwasremarkablydecreasedinadose-dependentmanner.户使⽤本产品发表的科研⽂献•Blood.2018Jul12;132(2):210-222.•SciTranslMed.2018Jul18;10(450).pii:eaaq1093.•JPinealRes.2019Apr;66(3):e12552.•NatCommun.2021Mar29;12(1):1940.•NatCommun.2019Jan28;10(1):453.Seemorecustomervalidationsonwww.MedChemEREFERENCES3/4www.MedChemEwww.MedChemE[1].ChaussadeC,etal.EvidenceforfunctionalredundancyofclassIAPI3Kisoforms.BiochemJ.2007Jun15;404(3):449-58.[2].GharbiSI,etal.ExploringthespecificityofthePI3KfamilyinhibitorLY294002.BiochemJ.2007May15;404(1):15-21.[3].DavidsonD,etal.SmallMolecules,InhibitorsofDNA-PK,TargetingDNARepair,andBeyond.FrontPharmacol.2013Jan31;4:5.[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.McePdfHeig