HSP90-mTOR-IN-1-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEHSP90/mTOR-IN-1Cat.No.:HY-151137分?式:C??H??ClFN?O?S分?量:717.21作?靶點(diǎn):mTOR;HSP;Apoptosis;Autophagy作?通路:PI3K/Akt/mTOR;CellCycle/DNADamage;MetabolicEnzyme/Protease;Apoptosis;Autophagy儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性HSP90/mTOR-IN-1?種有效的Hsp90和mTOR抑制劑，IC50分別為69nM和29nM。HSP90/mTOR-IN-1通過(guò)過(guò)度激活PI3K/AKT/mTOR通路抑制SW780細(xì)胞增殖。HSP90/mTOR-IN-1通過(guò)對(duì)HSP90和mTOR的選擇性抑制來(lái)誘導(dǎo)細(xì)胞凋亡(apoptosis)和細(xì)胞?噬(autophagy)。HSP90/mTOR-IN-1在異種移植??體內(nèi)也表現(xiàn)出良好的抗腫瘤活性。HSP90/mTOR-IN-1可?于膀胱癌的研究。IC50&TargetmTORHSP9029nM(IC50)69nM(IC50)體外研究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?邊的抑制劑?師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.體內(nèi)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?邊的抑制劑?師www.MedChemE[1].PanZ,etal.Design,synthesis,andbiologicalevaluationofnoveldualinhibitorsofheatshockprotein90/mammaliantargetofrapamycin(Hsp90/mTOR)againstbladdercancercells.EurJMedChem.2022Aug13;242:114674.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedic