| Identification | Back Directory | [Name]
LDN-214117 | [CAS]
1627503-67-6 | [Synonyms]
CS-1539
LDN-214117
LDN-214117;LDN214117
LDN-214117 USP/EP/BP
1-[4-[6-Methyl-5-(3,4,5-trimethoxyphenyl)-3-pyridinyl]phenyl]piperazine
1-(4-(6-methyl-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl)phenyl)piperazine
Piperazine, 1-[4-[6-methyl-5-(3,4,5-trimethoxyphenyl)-3-pyridinyl]phenyl]- | [Molecular Formula]
C25H29N3O3 | [MDL Number]
MFCD28168043 | [MOL File]
1627503-67-6.mol | [Molecular Weight]
419.52 |
| Chemical Properties | Back Directory | [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) | [form ]
Powder | [pka]
8.86±0.10(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [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 signalingand low cytotoxicity. LDN-214117 inhibited ALK2 mostwith a biochemical IC50 of 24 nMfollowed by TNIKRIPK2and 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. |
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