Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEZINC69391Cat.No.:HY-102078CASNo.:303094-67-9分?式:C??H??F?N?分?量:309.29作?靶點:Ras;Apoptosis作?通路:GPCR/GProtein;Apoptosis儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性ZINC69391?種特異的Rac1抑制劑，通過在Rac1表掩蔽Trp56殘來?擾Rac1-GEF的相互作?。ZINC69391?擾Rac1與Dock180的相互作?，降低Rac1-GTP?平。ZINC69391誘導(dǎo)細胞凋亡，具有抗增殖和抗轉(zhuǎn)移作?。體外研究ZINC69391inhibitsgrowthofU937,HL-60,KG1AandJurkatcellswithIC50srangingfrom41to54μM[1].ZINC69391(50-100μM;24hours)augmentstheenzymaticactivityofcaspase3inaconcentrationdependentmanner[1].ZINC69391(0-125μM;72h)reducescellproliferationofhumangliomacells[2].ZINC69391(50-100μM;48hours)triggerscellcyclearrest[2].ZINC69391(50μM;24hours)triggersapoptosisonhumanacuteleukemiccells[1].CellProliferationAssay[2]CellLine:U-87MG,LN229cellsConcentration:0-125μMIncubationTime:72hoursResult:Reducedcellproliferationinaconcentration-dependentmanner.CellCycleAnalysis[2]CellLine:LN229cells1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEConcentration:50,100μMIncubationTime:48hoursResult:Resultedinasignificantincreasedpercentageofcellsinthesub-G0/G1phaseinaconcentrationdependentmanner.ApoptosisAnalysis[1]CellLine:HL-60,U937andKG1AcelllinesConcentration:50μMIncubationTime:24hoursResult:Ledtoasignificantincreaseinapoptoticcells.體內(nèi)研究ZINC69391(25mg/kg;i.p;dailyfor21days)impairsmetastaticlungcolonizationinasyngeneicanimalmodel[3].AnimalModel:Specificpathogen-freefemaleBALB/cinbredmice(bearingF3IIcells)[3]Dosage:25mg/kgbodyweightAdministration:I.p;dailyfor21daysResult:Significantlyreducedbyabout60%theformationoftotalmetastaticlungcolonies.REFERENCES[1].CabreraM,etal.PharmacologicalRac1inhibitorswithselectiveapoptoticactivityinhumanacuteleukemiccelllines.Oncotarget.2017;8(58):98509‐98523.Published2017Oct4.[2].CardamaGA,etal.ProapoptoticandantiinvasiveactivityofRac1smallmoleculeinhibitorsonmalignantgliomacells.OncoTargetsTher.2014;7:2021‐2033.Published2014Oct30.[3].CardamaGA,etal.PreclinicaldevelopmentofnovelRac1-GEFsignalinginhibitorsusingarationaldesignapproachinhighlyaggressivebreastcancercelllines.AnticancerAgentsMedChem.2014;14(6):840‐851.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.For