LDN-212854 (1432597-26-6) Description:
LDN-212854 is an ALK2-Biased BMP Type I Receptor Kinase Inhibitor. LDN-212854 has some selectivity for ALK2 with an IC50 of 1.3 nM in preference to other BMP type I receptors, ALK1 (IC50=2.4 nM) and ALK3 (IC50=85.8 nM). LDN-212854 shows better selectivity than LDN193189 in cell-based assays of BMP signaling. LDN-212854 inhibited BMP6-induced osteogenic differentiation, which functions primarily via ALK2, more potently than BMP4, which functions primarily with ALK3 (IC50s of 10 nM versus 40.5 nM), whereas LDN-193189 inhibited both equally. The only off target effects found against a panel of 198 kinases were for RIPK2, ABL1, and PDGFR-β with IC50 values < 100 nM.
LDN-212854 is also known as 5-[6-[4-(1-Piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-quinoline. LDN-212854 prevents heterotopic ossification in an inducible mutant ALK2 (activin receptor-like kinase 2).
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).1 It has been shown to inhibit BMP6-induced osteogenic differentiation, which functions predominantly via ALK2, with an IC50 value of 10 nM.1 LDN-212854 also demonstrates off-target activity against RIPK2, ABL1, and PDGFRβ kinases with IC50 values less than 100 nM.1
LDN-212854 (1432597-26-6) Specifications:
|Synonyms||LDN 212854; LDN 212854;BMP Inhibitor III|
|Molecular Weight||406.493 g/mol|
|Monoisotopic Mass||406.191 g/mol|
|Color||white to beige|
|Solubility||Soluble in DMSO|
|Storage Temp.||0 – 4 C for short term (days to weeks), or -20 C for long term (months).|
|Shelf life||>2 years if stored properly|
|Handling||Protect from air and light|
|Application||BMP receptor inhibitor|