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.
Sold for research purposes under exclusive agreement from The Brigham and Women's Hospital Inc. US patent 14/776,302
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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|
References are publications that support the products' biological activity.
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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Keywords: LDN 214117, supplier, LDN214117, Inhibitors, Inhibits, ALK1, ALK2, BMP, Bone, morphogenic, protein, BMP6, TGF-, β1, TGF-b1, TGF-beta1, kinase, activin, receptor-like, kinases, BMP, and, Other, Activin, Receptors, BMP, and, Other, Activin, Receptors, Tocris Bioscience
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