LDN-214117 Chemical Properties

Boiling point:

567.9±50.0 °C(Predicted)

Density 

1.134±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMF:30.0(Max Conc. mg/mL);71.51(Max Conc. mM)
DMF:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);1.19(Max Conc. mM)
DMSO:42.67(Max Conc. mg/mL);101.7(Max Conc. mM)
Ethanol:54.0(Max Conc. mg/mL);128.72(Max Conc. mM)

pka

8.86±0.10(Predicted)

form 

Powder

color 

Light yellow to yellow

Safety Information

Hazard Codes 

T

Risk Statements 

25

Safety Statements 

45

LDN-214117 Usage And Synthesis

Uses

LDN 214117 is a highly selective ALK2 inhibitor.

Biological Activity

LDN-214117 is a selective inhibitor of the bone morphogenetic protein (BMP) type I receptor kinases with high selectivity for BMP versus TGF-β signaling, and low cytotoxicity. LDN-214117 inhibited ALK2 most, with a biochemical IC50 of 24 nM, followed by TNIK, RIPK2, and ABL1. LDN-214117 has a cell-based IC50 for BMP6 of approximately 100 nM and 164-fold selectivity for BMP6 versus TGF-β1. Fibrodysplasia ossificans progressiva (FOP) is a debilitating and progressive heterotopic ossification disease caused by activating mutations of ACVR1 encoding the BMP type I receptor kinase ALK2. LDN-214117 had nearly identical binding affinity for wild-type ALK2 and each of the FOP-causing mutants tested.

LDN-214117(1627503-67-6)Related Product Information

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