For research use only. Not for therapeutic Use.
Potent ALK2-biased BMP type I receptor kinase inhibitor (IC50 values 2.4 nM, 1.3 nM, and 85.8 nM for ALK1, 2, and 3 resp.), showing nearly 4 orders of selectivity for BMP versus the closely related TGF-β and Activin type I receptors. The free base form, LDN 212854 is available as Axon 3552. Closely related to LDN 193189 (Axon 1509).
KEYWORDS: LDN 212854 trihydrochloride | supplier | BMP inhibitor | LDN212854 | LDN-212854 | CAS [2109414-80-2] | [1432597-26-6] | TGF-β | BMP-ALK | ALK | type I | dorsomorphin | ALK2 | ALK-2 | ALK1 | ALK3 | bone morphogenetic protein | Antagonist | Receptors
| Catalog Number | I047601 |
| CAS Number | 2109414-80-2 |
| Molecular Formula | C25H22N6.3HCl |
| Purity | ≥95% |
| IUPAC Name | 5-[6-(4-piperazin-1-ylphenyl)pyrazolo[1,5-a]pyrimidin-3-yl]quinoline;trihydrochloride |
| InChI | InChI=1S/C25H22N6.3ClH/c1-3-21(22-4-2-10-27-24(22)5-1)23-16-29-31-17-19(15-28-25(23)31)18-6-8-20(9-7-18)30-13-11-26-12-14-30;;;/h1-10,15-17,26H,11-14H2;3*1H |
| SMILES | C1CN(CCN1)C2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=C6C=CC=NC6=CC=C5)N=C3.Cl.Cl.Cl |
| Reference | A.H. Mohedas et al. Development of an ALK2-Biased BMP Type I Receptor Kinase Inhibitor. ACS Chem. Biol. 2013. [Epub ahead of print].
D.W. Engers et al. Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of (…). Bioorg. Med. Chem. Lett. 2013, 23, 3248-3252. |
