A selective ALK1 and ALK2 inhibitor
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.
参考文献:
[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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