LDN-214117 |
| Catalog No.GC13225 |
Le LDN-214117 est un inhibiteur d'ALK2 actif par voie orale avec une pénétration cérébrale bien tolérée et bonne. LDN-214117 a une sélectivité élevée et une faible cytotoxicité pour ALK2 avec une valeur IC50 de 24 nM. Le LDN-214117 est également un inhibiteur spécifique de la signalisation des protéines morphogénétiques osseuses (BMP) et présente une inhibition relativement sélective de la BMP6 avec une valeur IC50 de 100 nM. LDN-214117 peut être utilisé pour la recherche sur la fibrodysplasie ossifiante progressive (FOP), le gliome pontique intrinsèque diffus (DIPG) up.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1627503-67-6
Sample solution is provided at 25 µL, 10mM.
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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.
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.
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