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PotentandselectiveinhibitoroftypeIbonemorphogenicprotein(BMP)receptorALK2(IC50=24nM).ShowspreferenceforALK1andALK2overALK3and164-foldselectivityforBMP6inhibition(IC50=100nM)overTGF-β1.ExhibitsimprovedkinomeselectivityoverK02288(Cat.No.4986)andlowcytotoxicity.
SoldforresearchpurposesunderexclusiveagreementfromTheBrighamandWomen"sHospitalInc.USpatent14/776,302
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight419.52.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Mohedasetal(2014)Structure-activityrelationshipof3,5-diaryl-2-aminopyridineALK2inhibitorsrevealsunalteredbindingaffinityforfibrodysplasiaossificansprogressivacausingmutants.JMedChem.577900PMID:25101911
Keywords:LDN214117,supplier,LDN214117,Inhibitors,Inhibits,ALK1,ALK2,BMP,Bone,morphogenic,protein,BMP6,TGF-,β1,TGF-b1,TGF-beta1,kinase,activin,receptor-like,kinases,BMP,and,Other,Activin,Receptors,BMP,and,Other,Activin,Receptors,TocrisBioscience
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