LDN-214117

  • Chemical Properties
CAS No. 1627503-67-6 Cat. No. BCP12392
Name LDN-214117
Synonyms LDN214117;LDN 214117;
Formula C25H29N3O3 M. Wt 419.52
  • Biological Activity
Description LDN-214117 inhibited ALK2 most, with a biochemical IC50 of 24 nM, followed by TNIK, RIPK2, and ABL1. LDN-214117 has a cell-based IC50 for BMP6 of approximately 100 nM and 164-fold selectivity for BMP6 versus TGF-β1. Fibrodysplasia ossificans progressiva (FOP) is a debilitating and progressive heterotopic ossification disease caused by activating mutations of ACVR1 encoding the BMP type I receptor kinase ALK2. LDN-214117 had nearly identical binding affinity for wild-type ALK2 and each of the FOP-causing mutants tested.
Pathways TGF beta/Smad  
Targets BMP/TGF beta Receptor 

Structure

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