740-Y-P-740YPDGFR-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemE740Y-PCat.No.:HY-P0175CASNo.:1236188-16-1Synonyms:740YPDGFR;PDGFR740Y-P分⼦式:C₁₄₁H₂₂₂N₄₃O₃₉PS₃分⼦量:3270.7SequenceShortening:RQIKIWFQNRRMKWKKSDGG-{PO2Y}-MDMS作⽤靶点:PI3K;Autophagy作⽤通路:PI3K/Akt/mTOR;Autophagy储存⽅式:ProtectfromlightPowder-80°C2years-20°C1yearInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:25mg/mL(7.64mM;Needultrasonic)H2O:2mg/mL(0.61mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM0.3057mL1.5287mL3.0574mL5mM0.0611mL0.3057mL0.6115mL10mM---------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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(protectfromlight)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。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：1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE(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%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(0.76mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(0.76mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(0.76mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性740Y-P(740YPDGFR;PDGFR740Y-P)⼀个有效的，具有细胞渗透性的PI3K激活剂。740Y-P很容易结合含有p85的N-和C-末端SH2结构域的GST融合蛋⽩，但不能单独结合GST。IC50&TargetPI3K体外研究740Y-P(50μg/mL;48hours)specificlystimulatesmitogenesisinmediumisbetterthanEGForFGFatstimulatingentryintoS-phase,itshowsthepercentageofcellsinS-phasefor48.3%inC2cells.Additionally,LY294002(HY-10108)orWortmannin(HY-10197)potentlyinhibitsthemitogenicresponsestimulatedbythepeptide[1].740Y-P(1μg/mL)stimulatesmitogenesisatthelowestconcentrationtested.Thepeptidestimulatesmitogenesisinboththepresenceandabsenceofserum(0.5%),andintheformerinstanceamaximalresponseobservedat50μg/mL.740Y-PtostimulatemitogenesisishighlyspecificandnotageneralfeatureofacellpermeableSH2domainbindingpeptides[1].740Y-P(30μM;24hours)remarkablyinhibitsthelevelofLC3-II/LC3-IinGO-inducedPC12cells[2].WesternBlotAnalysis[2]CellLine:PC12cellsConcentration:30μMIncubationTime:24hoursResult:InhibitedtheproteinexpressionofLC3-II.体内研究740Y-Pisnotonlyinternalisedinlivingcellsbutcanalsointeractwithp85invivo[1].740Y-P(intraperitonealinjection;10mg/kg;6weeks)decreasesthedegreeofROSlevelsinAβ(25-32)treatedhippocampaltissuesandincreasestheextentofAKTandPI3Kphosphorylationinalzheimer’sdisease(AD)ratmodel[3].户使⽤本产品发表的科研⽂献•MolCancer.2022May10;21(1):112.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•JClinInvest.2022Nov22;e153470.•Biomaterials.2019Feb;194:57-72.•JExpClinCancerRes.2021Aug12;40(1):255.•JExpClinCancerRes.2020Jun30;39(1):123.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].DerossiD,etal.Stimulationofmitogenesisbyacell-permeablePI3-kinasebindingpeptide.[2].XiaoliFeng,etal.GrapheneOxideInducesp62/SQSTM-dependentApoptosisThroughtheImpairmentofAutophagicFluxandLysosomalDysfunctioninPC12Cells.ActaBiomater.2018Nov;81:278-292.[3].ZhiqingSun,etal.GABABReceptor-MediatedPI3K/AktSignalingPathwayAlleviatesOxidativeStressandNeuronalCellInjuryinaRatModelofAlzheimer'sDisease.JAlzheimersDis.2020;76(4):1513-1526.McePdfHeightCaution:Producthas