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LDN 212854 trihydrochloride
- Parent CAS: 1432597-26-6
- Soluble in water and DMSO
- MF: C25H22N6.3HCl
- MW: 515.87
Description
LDN 212854 trihydrochloride is a potent ALK2-biased BMP type I receptor kinase inhibitor with reported IC50 values of 2.4 nM for ALK1, 1.3 nM for ALK2 and 85.8 nM for ALK3. It shows strong selectivity over TGF-β type I receptor signaling in reported profiling.
ALK2-mediated BMP signaling is implicated in developmental biology, stem-cell differentiation and disorders such as fibrodysplasia ossificans progressiva. LDN 212854 is relevant for probing ALK2-biased BMP pathway inhibition.
Key Features
- Potent ALK2-biased BMP receptor inhibitor
- Low-nanomolar activity against ALK1 and ALK2
- Selectivity over TGF-β receptor signaling reported
- Useful for BMP/SMAD pathway modulation
Applications
- ALK2 kinase assays
- BMP signaling research
- Stem cell differentiation studies
- Fibrodysplasia ossificans progressiva model research
Note: The free base form, LDN 212854 (Axon 3552) is available. It is a structural isomer of LDN 193189 (Axon 1509).
More Information
| Parent CAS No. | 1432597-26-6 |
|---|---|
| Chemical Name | 5-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline trihydrochloride |
| SMILES | N1C2C(=C(C3=C4N(N=C3)C=C(C3=CC=C(N5CCNCC5)C=C3)C=N4)C=CC=2)C=CC=1.Cl.Cl.Cl |
| MFCD | N.A. |
| 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 |
| InChiKey | RIMSXBSYXNLYPT-UHFFFAOYSA-N |
| CID | 91826503 |
| Short Description | BMP inhibitor |
References
- 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.
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