Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemERac1-IN-5Cat.No.:HY-175341CASNo.:694515-65-6分子式:C??H??N?O?S?分子量:486.6作用靶點:Acyltransferase;Ras;Akt作用通路:MetabolicEnzyme/Protease;GPCR/GProtein;MAPK/ERKPathway;PI3K/Akt/mTOR儲存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Rac1-IN-5是一種特異性的RAC1蛋白可逆抑制劑(KD=30nM)。Rac1-IN-5可與鳥嘌呤核苷酸在RAC蛋白上特異性結(jié)合競爭，有效阻斷RAC1活性和RAC1依賴性細(xì)胞功能。Rac1-IN-5在體內(nèi)表現(xiàn)出抗腫瘤轉(zhuǎn)移作用，并且可以提高生存率。Rac1-IN-5可用于研究侵襲性癌癥如三陰性乳腺癌，結(jié)腸癌[1]。體外研究Rac1-IN-5(CompoundA41)(10μM,1h)blocksRAC1activationandRAC1-dependentfunctionsinEGF-stimulatedNIH/3T3fibroblasts[1].Rac1-IN-5(10μM)reducestheactivityofRACP29SandRAC1binNIH-3T3fibroblastsexpressingRACwild-type(RAC1WT)orRAC1oncomutants(RAC1P29SandRAC1b)[1].Rac1-IN-5(0.01-10μM)reducesRAC1-GTPlevels,theover-activationofAKTandthemigrationareaofspheroids,inhibitscolonyformation(IC50=2.1μM)inTNBCMDA-MB-468luciferase(Luc)cells[1].Rac1-IN-5(10μM)hasanti-invasivepropertiesinhumanbreastCAFspheroids[1].WesternBlotAnalysis[1]CellLine:MDA-MB-468LuccellsConcentration:10μMIncubationTime:1hResult:ReducedAKToveractivation,whilep44/42activationremainedunchanged.體內(nèi)研究Rac1-IN-5(CompoundA41)(25mg/kg,i.p.,onceaday,4weeks)preventsmetastasisinamousemodelof1/2 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemETNBC[1].Rac1-IN-5(25mg/kg,i.p.,onceaday,15days)preventsmetastasisininvasivecancersinCT26cellsxenograftBALB/cfemalemicemodel[1].AnimalModel:TNBC(4millionMDA-MB-468Luccells)xenograftNMRInudemice(5-week-old)model[1]Dosage:25mg/kgAdministration:i.p.,onceaday,4weeksResult:Reducedprimarytumorregeneration,secondarytumorsinthefemur,lungs,kidneys,ovaries,anduterus,reducedexvivoluminescenceintensityintheovariesanduterus.AnimalModel:TNBC(4millionMDA-MB-468Luccells)xenograftBALB/cfemalemice(7-8-week-old)model[1]Dosage:25mg/kgAdministration:i.p.,onceaday,4weeksResult:Reducedthefrequencyofprimarytumorregrowthandmetastasis,improvingsurvivalrates.AnimalModel:CT26cells(1x106)xenograftBALB/cfemalemice(7-8-week-old)model[1]Dosage:25mg/kgAdministration:i.p.,onceaday,15daysResult:Reducedthedevelopmentoflungmetastasesandlivermetastases,improvingsurvivalrates.REFERENCESDilasserF,etal.ARac-specificcompetitiveinhibitorofguaninenucleotidebindingreducesmetastasisintriple-negativebreastcancer.CellRepMed.2025Jul15;6(7):102233.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplicatio