Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemE740Y-PCat.No.:HY-P0175CASNo.:1236188-16-1Synonyms:740YPDGFR;PDGFR740Y-P分?式:C???H???N??O??PS?分?量:3270.7SequenceShortening:RQIKIWFQNRRMKWKKSDGG-{PO2Y}-MDMS作?靶點(diǎn):PI3K;Autophagy作?通路:PI3K/Akt/mTOR;Autophagy儲(chǔ)存?式:ProtectfromlightPowder-80°C2years-20°C1yearInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:25mg/mL(7.64mM;Needultrasonic)H2O:2mg/mL(0.61mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM0.3057mL1.5287mL3.0574mL5mM0.0611mL0.3057mL0.6115mL10mM---------請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(protectfromlight)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(0.76mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(0.76mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(0.76mM);ClearsolutionBIOLOGICALACTIVITY?物活性740Y-P(740YPDGFR;PDGFR740Y-P)?個(gè)有效的，具有細(xì)胞滲透性的PI3K激活劑。740Y-P很容易結(jié)合含有p85的N-和C-末端SH2結(jié)構(gòu)域的GST融合蛋?，但不能單獨(dú)結(jié)合GST。IC50&TargetPI3K體外研究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.體內(nèi)研究740Y-Pisnotonlyinternalisedinlivingcellsbutcanalsointeractwithp85invivo[1].740Y-P(intraperitonealinjection;10mg/kg;6weeks)decreasesthedegreeofROSlevelsinAβ(25-32)treatedhippocampaltissuesandincreasestheextentofAKTandPI3Kphosphorylationinalzheimer’sdisease(AD)ratmodel[3].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?MolCancer.2022May10;21(1):112.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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