CRT0066101-trihydrochloride-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECRT0066101trihydrochlorideCat.No.:HY-15698BCASNo.:1781742-22-0分⼦式:C₁₈H₂₅Cl₃N₆O分⼦量:447.79作⽤靶点:PKD;Pim;Apoptosis作⽤通路:Apoptosis;JAK/STATSignaling储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性CRT0066101trihydrochlorideCRT0066101(HY-15698)的三盐酸盐形式。CRT0066101trihydrochloridePKD抑制剂，对PKD1、PKD2和PKD3的IC50值分别为1nM、2.5nM和2nM。CRT0066101trihydrochloride也⼀种有效的PIM2抑制剂，IC50约为135.7nM。CRT0066101trihydrochloride在LPS(HY-D1056)诱发的⼩⿏肺损伤模型中表现出抗炎活性。CRT0066101trihydrochloride具有抗癌作⽤。IC50&TargetPKD1PKD3PKD2PIM21nM(IC50)2nM(IC50)2.5nM(IC50)135.7nM(IC50)体外研究CRT0066101trihydrochloride(5µM;1h)blockSboththebasalandNT-inducedpS916-PKD1/2(activatedPKD1/2)inPanc-1andPanc-28cells.CRT0066101abrogatesNT-inducedphosphorylationofHsp27(pS82-Hsp27),attenuatesPKD1-mediatedNF-κBactivation,andabrogatesexpressionofNF-κB-dependent-dependentproliferativeandpro-survivalproteins[1].CRT0066101trihydrochloridesignificantlyinhibitsPanc-1cellproliferation,withanIC50valueof1µM.CRT0066101trihydrochlorideresultsina6-10foldinductionofapoptosisinPanc-1cells.CRT0066101trihydrochloridesignificantlyreducescellproliferationofColo357,Panc-1,MiaPaCa-2,andAsPC-1cellsbuthadamodesteffectinCapan-2cells[1].WesternBlotAnalysis[1]CellLine:Panc-1andPanc-28cellsstimulationwithneurotensin(NT)Concentration:5µM1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEIncubationTime:1hResult:BlockedboththebasalandNT-inducedpS916-PKD1/2(activatedPKD1/2).体内研究CRT0066101trihydrochloride(80mg/kg/day;oralgavage;oncedaily;for21days)inPanc-1orthotopicmodelpotentlyblockstumorgrowthinvivo[1].CRT0066101trihydrochloride(10mg/kg,i.p.,everytwodaysfor3times)exhibitsaprotectiveeffectagainstLPS-inducedpneumoniaandalleviateslungdamageinC57BL/6Jmice[3].AnimalModel:CR-UKnu/numiceinjectedwithPanc-1cells[1]Dosage:80mg/kg/dayAdministration:Oralgavage;oncedaily;for21daysResult:Potentlyblockedtumorgrowthinvivo.AnimalModel:LPS(HY-D1056)-inducedlunginjuryinC57BL/6Jmice[3]Dosage:10mg/kgAdministration:i.p.,onceeverytwodaysfor3timesResult:InhibitedtheexpressionofMyD88andTLR4,inhibitedthephosphorylationofNF-κB,ERKandJNK.•ExpMolMed.2022Sep21.•IntImmunopharmacol.2023May12;120:110240.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].HarikumarKB,etal.Anovelsmall-moleculeinhibitorofproteinkinaseDblockspancreaticcancergrowthinvitroandinvivo.MolCancerTher.2010May;9(5):1136-46.[2].XiChen,etal.IdentificationandassessmentofnewPIM2inhibitorsfortreatinghematologiccancers:Acombinedapproachofenergy-basedvirtualscreeningandmachinelearningevaluation.ArchPharm(Weinheim).2024Jan23:e2300516.[3].CuiB,etal.,SmallmoleculeinhibitorCRT0066101inhibitscytokinestormsyndromeinamousemodeloflunginjury.IntImmunopharmacol.2023Jul;120:110240.McePdfHeight2/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyv