LDN-212854 |
| カタログ番号GC17035 |
LDN-212854 は、ALK2 を強力に阻害する骨形成タンパク質 (BMP) 阻害剤です (IC50: 1.3 nM)。 LDN-212854 は ALK1 も阻害します (IC50: 2.40 nM)。 LDN-212854 は、進行性骨化性線維異形成症および肝細胞癌 (HCC) などの癌の研究に使用できます。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1432597-26-6
Sample solution is provided at 25 µL, 10mM.
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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.
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