KS-501-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEKS501Cat.No.:HY-117232CASNo.:120634-86-8分⼦式:C₃₃H₄₈O₁₀分⼦量:604.73作⽤靶点:Calmodulin作⽤通路:MembraneTransporter/IonChannel储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性KS501⼀种强效且选择性的钙调蛋⽩(calmodulin)抑制剂。KS501可抑制钙调蛋⽩激酶I和II的活化，但对环磷酸腺苷(cAMP)敏感激酶的响较⼩。KS501的抑制作⽤并⾮直接作⽤于酶本⾝，⽽通过⼲扰钙调蛋⽩的活化来实现的。KS501可⽤于⽩⾎病的研究[1]。体外研究KS501(0-100μM)inhibitscalmodulin-sensitivephosphodiesteraseactivityinaconcentration-dependentmanner(IC50=0.8μM)[1].KS501(0.25-2μM)showsadecreasinginhibitoryeffectonphosphodiesteraseactivityastheconcentrationofcalmodulinincreases[1].KS501(10-40μM)inhibitscalmodulin-dependentsynapsinIphosphorylationat40μM,while10μMhasnoinhibitoryeffectonbasalactivityandinsteadcausesslightstimulation[1].KS501(10-40μM)inhibitsthephosphorylationofsynapsinIatsite1(asubstrateofcalmodulinkinaseI)andsites2and3(asubstrateofcalmodulinkinaseII)[1].KS501(10-40μM)onlypartiallyinhibitssynapsinIphosphorylationofcAMP-sensitiveproteinkinase(PKA)[1].KS501(0-120μM)inhibitstheproliferationofL1210/Scells(IC50=80μM)[1].REFERENCES[1].HaitWN,etal.EffectsofKS-501,KS-502andtheirenantiomersoncalmodulin-sensitiveenzymeactivityandcellularproliferation.BiochemPharmacol.1995Jun29;50(1):69-74.McePdfHeight1/1MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;021-589559