LDN-212854

An ALK2 inhibitor

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库存: 现货

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5mg

￥850.00

680.00

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10mg

￥1462.00

1170.00

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50mg

￥4962.00

3970.00

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货号: ajci18312
CAS: 1432597-26-6
别名: 5-（6-（4-（哌嗪-1-基）苯基）吡唑并[1,5-a]嘧啶-3-基）喹啉
分子式: C25H22N6
分子量: 406.48
纯度: >98%
溶解度: ≥ 20.3mg/mL in DMSO
储存: Store at -20°C
库存: 现货

Background

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].

参考文献:
[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.