LDN 214117

Modify Date: 2024-01-10 13:07:45

LDN 214117 Structure
LDN 214117 structure
Common Name LDN 214117
CAS Number 1627503-67-6 Molecular Weight 419.516
Density 1.1±0.1 g/cm3 Boiling Point 567.9±50.0 °C at 760 mmHg
Molecular Formula C25H29N3O3 Melting Point N/A
MSDS N/A Flash Point 297.3±30.1 °C

 Use of LDN 214117


LDN-214117 is a potent and selective ALK2 inhibitor with IC50 of 22 nM; > 100 fold selectivity for ALK5; also inhibits BMP6(IC50=100 nM).IC50 value: 22 nM(ALK2) [1]Target: ALK2 inhibitorLDN-214117 is a highly BMP selective compound, significantly biased toward ALK2 and its cognate ligands including BMP6 and also demonstrates a high degree of kinome selectivity and lowcytotoxicity. LDN-214117 may be useful as highly selectiveprobes of BMP-mediated cellular physiology that may provide auseful complement to the dorsomorphin class of compounds. Furthermore, this class of BMP inhibitors offers a structurallydistinct template for the development of therapeutics for thetreatment of BMP signaling-mediated diseases such as FOP.

 Names

Name 1-{4-[6-Methyl-5-(3,4,5-trimethoxyphenyl)-3-pyridinyl]phenyl}piperazine
Synonym More Synonyms

 LDN 214117 Biological Activity

Description LDN-214117 is a potent and selective ALK2 inhibitor with IC50 of 22 nM; > 100 fold selectivity for ALK5; also inhibits BMP6(IC50=100 nM).IC50 value: 22 nM(ALK2) [1]Target: ALK2 inhibitorLDN-214117 is a highly BMP selective compound, significantly biased toward ALK2 and its cognate ligands including BMP6 and also demonstrates a high degree of kinome selectivity and lowcytotoxicity. LDN-214117 may be useful as highly selectiveprobes of BMP-mediated cellular physiology that may provide auseful complement to the dorsomorphin class of compounds. Furthermore, this class of BMP inhibitors offers a structurallydistinct template for the development of therapeutics for thetreatment of BMP signaling-mediated diseases such as FOP.
Related Catalog
References

[1]. Mohedas AH, et al. Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. J Med Chem. 2014 Oct 9;57(19):7900-15.

 Chemical & Physical Properties

Density 1.1±0.1 g/cm3
Boiling Point 567.9±50.0 °C at 760 mmHg
Molecular Formula C25H29N3O3
Molecular Weight 419.516
Flash Point 297.3±30.1 °C
Exact Mass 419.220886
LogP 3.27
Vapour Pressure 0.0±1.6 mmHg at 25°C
Index of Refraction 1.573
Storage condition 2-8°C

 Safety Information

Hazard Codes T
Risk Phrases 25
Safety Phrases 45

 Synonyms

1-{4-[6-Methyl-5-(3,4,5-trimethoxyphenyl)-3-pyridinyl]phenyl}piperazine
Piperazine, 1-[4-[6-methyl-5-(3,4,5-trimethoxyphenyl)-3-pyridinyl]phenyl]-
LDN-214117
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