Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemECLM296Cat.No.:HY-174209CASNo.:3067837-25-3分子式:C??H??N?O?分子量:430.5作用靶點(diǎn):AldehydeDehydrogenase(ALDH)作用通路:MetabolicEnzyme/Protease儲(chǔ)存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性CLM296是一種強(qiáng)效且選擇性的ALDH1A3抑制劑，其IC50為2nM。CLM296對(duì)高度同源的ALDH1A1異構(gòu)體沒有脫靶效應(yīng)。CLM296可抑制ALDH1A3驅(qū)動(dòng)的乳腺癌腫瘤轉(zhuǎn)移。CLM296可用于研究三陰性乳腺癌(TNBC)[1]。IC50&TargetALDH1A32nM(IC50)體外研究CLM296(0.01nM-10μM)significantlyreducesAldefluorTM438fluorescenceinMDA-MB-231cellswithALDH1A3overexpression,MDA-MB-468andHCC1806shRNAcontrolcellswithIC50valuesof2.1nM,2.5nM,and2.3nM,respectively[1].CLM296(1μM;72h)doesnotaffectcelldeathorproliferationinMDA-MB-231,MDA-MB-468orHCC1806cells[1].CLM296(100nM;24h)specificallyreducestheincreasedinvasionimpartedbyALDH1A3overexpressioninMDA-MB-231cells[1].CLM296(1-100nM;24h)specificallyblocksALDH1A3-mediatedgeneexpressionchangesinMDA-MB-231cells[1].CellViabilityAssay[1]CellLine:MDA-MB-231,MDA-MB-468andHCC1806cellsConcentration:1μMIncubationTime:72h1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEResult:Results:DidnotaffectcelldeathorproliferationinMDA-MB-231,MDA-MB-468orHCC1806cells.CellInvasionAssay[1]CellLine:MDA-MB-231cellsConcentration:100nMIncubationTime:24hResult:SpecificallyreducedtheincreasedinvasionimpartedbyALDH1A3overexpressioninMDA-MB-231cells.RT-PCR[1]CellLine:MDA-MB-231cellsConcentration:1nM,10nM,100nMIncubationTime:24hResult:SignificantlyreducedexpressionofALDH1A3-inducedgenes,RARβ,ELF3,andDHRS3.體內(nèi)研究CLM296(0-4mg/kg;intraperitoneal(IP)injection;oncedaily;for42days;12or15daysaftercellinjection)significantlyreducestumorvolumesandmetastasisinthemicebearingtumorswithALDH1A3overexpression[1].AnimalModel:Femalenon-obesediabeticseverecombinedimmunodeficient(NOD-SCID)mice(6-12weeksold)wereorthotopicallyimplantedwithMDA-MB-231cells(2x106)[1].Dosage:0mg/kg,0.4mg/kg,or4mg/kgAdministration:Intraperitoneal(IP)injection;oncedaily;for42days;15daysaftercellinjectionResult:SignificantlyreducedtumorvolumesinonlythemicebearingtumorswithALDH1A3overexpression.AnimalModel:Femalenon-obesediabeticseverecombinedimmunodeficient(NOD-SCID)mice(6-12weeksold)wereorthotopicallyimplantedwithMDA-MB-231cells(2x106)[1].Dosage:0mg/kg,0.4mg/kg,or4mg/kgAdministration:Intraperitoneal(IP)injection;oncedaily;for42days;12daysaftercellinjectionResult:ReducedmetastasisintheMDA622MB-231modelwithALDH1A3overexpression.2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEREFERENCESMayaRMacLean,etal.CLM296:ahighlyselectiveinhibitortargetingALDH1A3-driventumorgrowthandmetastasisinbreastcancer.bioRxiv.April18,2025.McePdfHeightCaution:Producthasnotbeenfullyvalidatedform