HSP90-mTOR-IN-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEHSP90/mTOR-IN-1Cat.No.:HY-151137分⼦式:C₃₆H₃₄ClFN₆O₅S分⼦量:717.21作⽤靶点:mTOR;HSP;Apoptosis;Autophagy作⽤通路:PI3K/Akt/mTOR;CellCycle/DNADamage;MetabolicEnzyme/Protease;Apoptosis;Autophagy储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性HSP90/mTOR-IN-1⼀种有效的Hsp90和mTOR抑制剂，IC50分别为69nM和29nM。HSP90/mTOR-IN-1通过过度激活PI3K/AKT/mTOR通路抑制SW780细胞增殖。HSP90/mTOR-IN-1通过对HSP90和mTOR的选择性抑制来诱导细胞凋亡(apoptosis)和细胞⾃噬(autophagy)。HSP90/mTOR-IN-1在异种移植⼩⿏体内也表现出良好的抗肿瘤活性。HSP90/mTOR-IN-1可⽤于膀胱癌的研究。IC50&TargetmTORHSP9029nM(IC50)69nM(IC50)体外研究HSP90/mTOR-IN-1(compound17o)hasantiproliferativeactivityagainstJ82,T24andSW780cells[1].HSP90/mTOR-IN-1(0.2and0.5μM;24h)inducesSW870apoptosisinadose-dependentmanner,inducestheformationofautophagosome[1].HSP90/mTOR-IN-1(0.2and0.5μM;24h)decreasestheexpressionofseveralHsp90clientproteinsinSW870[1].CellProliferationAssay[1]CellLine:J82,T24andSW780[1]Concentration:0-1μMIncubationTime:48hResult:ExhibitedantiproliferativeactivityagainstJ82,T24andSW780withIC50sof0.36±0.03μM,0.41±0.06μM,0.16±0.03μM.ApoptosisAnalysis[1]1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellLine:SW870Concentration:0.2and0.5μMIncubationTime:24hResult:Inducedapoptosisinadose-dependentmanner(totalapoptoticcellpercentagewas12.4%and16.5%at0.2and0.5μM,respectively).CellAutophagyAssay[1]CellLine:SW870(transfectedwithGFP-LC3)Concentration:0.2and0.5μMIncubationTime:24hResult:Inducedtheformationofautophagosome.Thegreenfluorescentspotswereobservedtoincreaseinthenumberandgathered.WesternBlotAnalysis[1]CellLine:SW870Concentration:0.2and0.5μMIncubationTime:24hResult:SignificantlydecreasedtheexpressionofseveralHsp90clientproteins,CDK4,C-RafandCDC2.体内研究HSP90/mTOR-IN-1(30mg/kg;PO;for17days)exhibitssignificantlysuperiortumorgrowthinhibitioninJ82xenograftmice[1].AnimalModel:Balc/cnudemice(6-8weeks;subcutaneouslyinjectedwith1×106cellsper100μLofJ82cellsintothemice'sdorsalskin)[1]Dosage:30mg/kgAdministration:PO;for17daysResult:Exhibitedsignificantlysuperiortumorgrowthinhibition,anddidnotshowedremarkableweightdecline.Inhibitedbladdercancercellproliferation,inducedcellapoptosis,degradedHsp70,aswellasdecreasedphosphorylationlevelsofmTORandincreasedexpressionofLC3-II.REFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].PanZ,etal.Design,synthesis,andbiologicalevaluationofnoveldualinhibitorsofheatshockprotein90/mammaliantargetofrapamycin(Hsp90/mTOR)againstbladdercancercells.EurJMedChem.2022Aug13;242:114674.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedic