LDN 214117 - ≥98%(HPLC), high purity , CAS No.1627503-67-6, Inhibitor of activin A receptor type 1;Inhibitor of activin A receptor type IL;Inhibitor of bone morphogenetic protein receptor type IA;Inhibitor of transforming growth factor beta receptor 1
LDN 214117 - ≥98%(HPLC), high purity , CAS No.1627503-67-6, Inhibitor of activin A receptor type 1;Inhibitor of activin A receptor type IL;Inhibitor of bone morphogenetic protein receptor type IA;Inhibitor of transforming growth factor beta receptor 1
Potent and selective inhibitor of type I bone morphogenic protein (BMP) receptor ALK2 (IC50= 24 nM). Shows preference for ALK1 and ALK2 over ALK3 and 164-fold selectivity for BMP6 inhibition (IC50= 100 nM) over TGF-β1. Exhibits improved kinome selectivity
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of activin A receptor type 1;Inhibitor of activin A receptor type IL;Inhibitor of bone morphogenetic protein receptor type IA;Inhibitor of transforming growth factor beta receptor 1
1.Shore EM, Xu M, Feldman GJ, Fenstermacher DA, Cho TJ, Choi IH, Connor JM, Delai P, Glaser DL, LeMerrer M et al.. (2006) A recurrent mutation in the BMP type I receptor ACVR1 causes inherited and sporadic fibrodysplasia ossificans progressiva.. Nat Genet, 38 (5):(525-7). [PMID:16642017][10.1021/op500134e]
2.Kaplan FS, Xu M, Seemann P, Connor JM, Glaser DL, Carroll L, Delai P, Fastnacht-Urban E, Forman SJ, Gillessen-Kaesbach G et al.. (2009) Classic and atypical fibrodysplasia ossificans progressiva (FOP) phenotypes are caused by mutations in the bone morphogenetic protein (BMP) type I receptor ACVR1.. Hum Mutat, 30 (3):(379-90). [PMID:19085907][10.1021/op500134e]
4.Nakahara Y, Katagiri T, Ogata N, Haga N. (2014) ACVR1 (587T>C) mutation in a variant form of fibrodysplasia ossificans progressiva: second report.. Am J Med Genet A, 164A (1):(220-4). [PMID:24259422][10.1021/op500134e]
5.Mohedas AH, Wang Y, Sanvitale CE, Canning P, Choi S, Xing X, Bullock AN, Cuny GD, Yu PB. (2014) Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants.. J Med Chem, 57 (19):(7900-15). [PMID:25101911][10.1021/op500134e]
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