Cayman LDN-212854

Activation of bone morphogenetic protein (BMP) type I receptors, also known as activin receptor-like kinases (ALK1-7), leads to the assembly of SMAD complexes, which translocate to the nucleus to induce transcriptional activation important for normal development and tissue repair. LDN-212854 inhibits ALK2 (IC₅₀ = 1.3 nM) in preference to other BMP type I receptors, ALK1 (IC₅₀ = 2.4 nM) and ALK3 (IC₅₀ = 85.8 nM) and with over 1,500-fold selectivity against the closely related activin and TGF-β type I receptors (i.e., ALK4 and ALK5). It has been shown to inhibit BMP6-induced osteogenic differentiation, which functions predominantly via ALK2, with an IC₅₀ value of 10 nM. LDN-212854 also demonstrates off-target activity against RIPK2, ABL1, and PDGFRβ kinases with IC₅₀ values less than 100 nM.

WARNING This product is not for human or veterinary use.