GLI1-IN-1-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEGLI1-IN-1Cat.No.:HY-161459CASNo.:2923907-92-8分子式:C₄₂H₆₀N₂O₉分子量:736.93作用靶点:Apoptosis;Hedgehog;Gli作用通路:Apoptosis;StemCell/Wnt储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性GLI1-IN-1(CBC-1)是GLI-1抑制剂，具有良好的水溶性和抗癌活性。GLI1-IN-1可以诱导细胞凋亡(apoptosis)，并且通过抑制Hedgehog(HH)(IC50=1.3μM)通路来抑制结直肠癌的生长[1]。IC50&TargetIC50:1.3μM(Hedgehog)[1].体外研究GLI1-IN-1(CBC-1)(5-40μM;24-48h)exhibitsanticanceractivitybyinhibitingcellproliferationthroughsuppressingthemRNAandproteinexpressionoftheHHpathwayinHT-29,SW-480,andHCT-116cells,withIC50valuesof7.13,15.31,and3.33μM,respectively.GLI1-IN-1(5-40μM;24h)canalsoinduceapoptosisinHT-29cells[1].ApoptosisAnalysis[1]CellLine:HT-29Concentration:5,10,20,40µM;IncubationTime:24hResult:Increasedthenumberofapoptoticcellsinaconcentration-dependentmanner.RT-PCR[1]CellLine:HT-29Concentration:5,10,20,40µM;1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEIncubationTime:24h,48hResult:DecreasedthemRNAexpressionofSHH,SMO,GLI1,andPTCHinaconcentration-andtime-dependentmanner.SignificantlyreducedthemRNAexpressionlevelsoftheapoptosis-relatedfactorBCL-2andincreasedthelevelsoftheapoptosis-promotingfactorBAXinadose-dependentmanner.WesternBlotAnalysis[1]CellLine:HT-29Concentration:5,10,20,40µM;IncubationTime:24hResult:DecreasedtheproteinexpressionofSHH,SMOandGLI1inaconcentration-dependentmanner.体内研究CBC-1(50mg/kg;i.p.;oncedailyfor16days)caneffectivelyinhibittumorgrowthinxenograftmodels,witharemarkabletumorinhibitionrateof68%inBALB/c/nu/nunudemice[1].AnimalModel:TumourxenograftBALB/c/nu/nunudemicemodel[1].Dosage:50mg/kgAdministration:Intraperitonealinjection(i.p.);Oncedailyfor16daysResult:SignificantlyreducedthesizeandweightofHT29tumorxenografts.DecreasedtheproteinexpressionofGLI-1.REFERENCESChenJ,etal.CBC-1asaCynanbungeigeninCderivativeinhibitsthegrowthofcolorectalcancerthroughtargetingHedgehogpathwaycomponentGLI1.Steroids.PublishedonlineApril11,2024.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchu