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LDN-212854 BMP receptor inhibitor,potent and selective

Catalog No.B3687
Size Price Stock Qty
10mM (in 1mL DMSO)
$112.00
In stock
5mg
$90.00
In stock
10mg
$180.00
In stock
50mg
$720.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

LDN-212854

Biological Activity

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          

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Chemical Properties

Cas No. 1432597-26-6 SDF Download SDF
Canonical SMILES C1CN(CCN1)C2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=C6C=CC=NC6=CC=C5)N=C3
Formula C25H22N6 M.Wt 406.48
Solubility >20.3mg/mL in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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].

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.