LDN 214117

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Cat.No. 6152 - LDN 214117 | C25H29N3O3 | CAS No. 1627503-67-6
Description: Potent and selective ALK2 inhibitor
Chemical Name: 1-[4-[6-Methyl-5-(3,4,5-trimethoxyphenyl)-3-pyridinyl]phenyl]piperazine
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature
Pathways

Biological Activity

Potent and selective inhibitor of type I bone morphogenic protein (BMP) receptor ALK2 (IC50 = 24 nM). Shows preference for ALK1 and ALK2 over ALK3 and 164-fold selectivity for BMP6 inhibition (IC50 = 100 nM) over TGF-β1. Exhibits improved kinome selectivity over K 02288 (Cat.No. 4986) and low cytotoxicity.

Licensing Information

Sold for research purposes under exclusive agreement from The Brigham and Women's Hospital Inc. US patent 14/776,302

Technical Data

M. Wt 419.52
Formula C25H29N3O3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1627503-67-6
PubChem ID 91754554
InChI Key BHUXVRVMMYAXKN-UHFFFAOYSA-N
Smiles COC1=CC(C2=C(N=CC(C3=CC=C(N4CCNCC4)C=C3)=C2)C)=CC(OC)=C1OC

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 41.95 100
ethanol 41.95 100

Preparing Stock Solutions

The following data is based on the product molecular weight 419.52. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.38 mL 11.92 mL 23.84 mL
5 mM 0.48 mL 2.38 mL 4.77 mL
10 mM 0.24 mL 1.19 mL 2.38 mL
50 mM 0.05 mL 0.24 mL 0.48 mL

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References

References are publications that support the biological activity of the product.

Mohedas et al (2014) Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. J Med Chem. 57 7900 PMID: 25101911


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View all BMP and Other Activin Receptor Inhibitors

Keywords: LDN 214117, LDN 214117 supplier, LDN214117, Inhibitors, Inhibits, ALK1, ALK2, BMP, Bone, morphogenic, protein, BMP6, TGF-, β1, TGF-b1, TGF-beta1, kinase, activin, receptor-like, kinases, and, Other, Activin, Receptors, 6152, Tocris Bioscience

Citations for LDN 214117

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Literature in this Area

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Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases

Pathways for LDN 214117

TGF-β

TGF-β Signaling Pathway

The TGF-β signaling pathway is involved in the regulation of growth and proliferation of cells along with migration, differentiation and apoptosis.