PAK4-IN-5-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPAK4-IN-5Cat.No.:HY-159897分⼦式:C₃₁H₂₈ClN₅O分⼦量:522.04作⽤靶点:PAK;LIMKinase(LIMK);Apoptosis;ReactiveOxygenSpecies作⽤通路:CellCycle/DNADamage;Cytoskeleton;Apoptosis;Immunology/Inflammation;MetabolicEnzyme/Protease;NF-κB储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性PAK4-IN-5(Compound12i)⼀种PAK4抑制剂(IC50:PAK4为7.68nM，PAK1为1872.01nM)。PAK4-IN-5通过多种相互作⽤稳定地与PAK4结合。PAK4-IN-5通过抑制PAK4和LIMK1的磷酸化来抑制MDA-MB-231细胞的增殖和迁移潜⼒。PAK4-IN-5将细胞周期停滞在G0/G1期，诱导细胞凋亡(Apoptosis)和活性氧产⽣。LD50：⼩⿏>500mg/kg(⼝服)。IC50&TargetPAK4PAK17.68nM(IC50)1872.01nM(IC50)体外研究PAK4-IN-5inhibitscellproliferationwithIC50sof1.87(A-549),1.56(NCI-H1975),1.21(MDA-MB-231),2.33(SK-BR-3),28.68μM(Beas-2B),26.68μM(MCF-10A),respectively[1].REFERENCES[1].HaoS,etal.Design,synthesisandbiologicalevaluationofnovelbenzimidazole-derivedp21-activitedkinase4(PAK4)inhibitorsbearinga4-(4-methylpiperazin-1-yl)phenylscaffoldaspotentialantitumoragents.EurJMedChem.2024Oct17;280:116971.[2].MengFH.Design,synthesisandbiologicalevaluationofnovelbenzimidazole-derivedp21-activitedkinase4(PAK4)inhibitorsbearinga4-(4-methylpiperazin-1-yl)phenylscaffoldaspotentialantitumoragents.EurJMedChem.2024Oct17;280:116971.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792ax