GLUT4-IN-2-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGLUT4-IN-2Cat.No.:HY-146980CASNo.:2454113-83-6分?式:C??H??N?O?S?分?量:385.42作?靶點(diǎn):Apoptosis;GLUT作?通路:Apoptosis;MembraneTransporter/IonChannel儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性GLUT4-IN-2?種有效的選擇性GLUT4抑制劑，對(duì)GLUT1和GLUT4的IC50s分別為11.4μM和6.8μM。GLUT4-IN-2誘導(dǎo)細(xì)胞凋亡(apoptosis)和細(xì)胞周期停滯在G0/G1期。GLUT4-IN-2顯?出有效的抗腫瘤活性[1]。IC50&TargetGLUT1GLUT411.4μM(IC50)6.8μM(IC50)體外研究GLUT4-IN-2(compoundF18)inducescellapoptosisandellcyclearrestatG0/G1phaseinCMEcells[1].GLUT4-IN-2(10μM;6h)decreasestheexpressionofmTORandCDK2,butincreasestheexpressionofGRP78,andcleavedcaspase3proteins[1].CellViabilityAssay[1]CellLine:CME,K562,KCL-22,MB-231,HS-27cellsConcentration:1-100μMIncubationTime:48hResult:Showedpotentcytotoxicitywithcytotoxicconcentration50%(CC50)of1.7,91.9,15.3,45.1,44.0μMforCME,K562,KCL-22,MB-231,HS-27cells,respectively.ApoptosisAnalysis[1]CellLine:CEMcells1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEConcentration:1.7μMIncubationTime:24hResult:Inducedcellapoptosiswiththepercentageofapoptoticcellsinthelateandearlyapoptosisregionwas55.87%and1.38%,respectively.CellCycleAnalysis[1]CellLine:CEMcellsConcentration:10,25,50μMIncubationTime:72hResult:InducedcellcyclearrestatG0/G1phaseinadose-dependentmanner.WesternBlotAnalysis[1]CellLine:CEMcellsConcentration:10μMIncubationTime:6hResult:DecreasedthephosphorylationofmTORandCDK2proteinsandincreasedtheexpressionofGRP78,andcleavedcaspase3.CellCytotoxicityAssay[1]CellLine:CEMcellsConcentration:2.5-100μMIncubationTime:48hResult:ShowedcytotoxicitywiththeIC50sof1.7,187.2μMforCEM,WBCscellsrespectively.體內(nèi)研究GLUT4-IN-2(50mg/kg;i.p.onday1–5,8–12,15–18)showsantitumoractivityinCEMxenograftmodel[1].AnimalModel:8–10weeks,SCIDmice(CEMxenografttumor)[1]Dosage:50mg/kgAdministration:I.p.;administeredonday1-5,8-12,15-18Result:Showedpotentantitumoractivityinvivo.REFERENCES2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[1].TilekarK,etal.StructureguideddesignandsynthesisoffurylthiazolidinedionederivativesasinhibitorsofGLUT1andGLUT4,andevaluationoftheiranti-leukemicpotential.EurJMedChem.2020Sep15;202:112603.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.For