LDN-212854
LDN-212854 is a selective inhibitor of bone morphogenetic protein (BMP) signaling with IC50 value of 1.2nM [1].
In the kinase assay, LDN-212854 shows inhibitory activities against caALK2 and caALK5 with IC50 values of 16nM and 2μM, respectively. It demonstrates that LDN-212854 is selective against BMP over TGF-β signaling. Besides that, the inhibition of caALK2 caused by LDN-212854 is 6- and 10-fold more potent than that of caALK1 and caALK3, respectively. In C2C12 cells transfected with BMP receptors, LDN-212854 also exerts preferential inhibition against caALK2. Furthermore, in a transgenic ALK2Q207D model of heterotopic ossification, treatment of LDN-212854 prevents the formation of heterotopic bone and preserves limb range of motion [1].
References:
[1] Mohedas A H, Xing X, Armstrong K A, et al. Development of an ALK2-biased BMP type I receptor kinase inhibitor. ACS chemical biology, 2013, 8(6): 1291-1302.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 406.48 |
| Cas No. | 1432597-26-6 |
| Formula | C25H22N6 |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥20.3 mg/mL in DMSO |
| SDF | Download SDF |
| Canonical SMILES | C(C1)NCCN1c(cc1)ccc1-c1c[n]2ncc(-c3cccc4c3cccn4)c2nc1 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Description | LDN-212854 is a potent and selective inhibitor of BMP receptor with IC50 of 1.3 nM for ALK2. | |||||
| Targets | ALK2 | |||||
| IC50 | 1.3 nM | |||||
Quality Control & MSDS
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Chemical structure
