LDN-214117 |
| رقم الكتالوجGC13225 |
LDN-214117 هو مثبط ALK2 نشط عن طريق الفم مع اختراق جيد للدماغ جيد التحمليحتوي LDN-214117 على انتقائية عالية وسمية خلوية منخفضة لـ ALK2 بقيمة IC50 تبلغ 24 نانومتريعد LDN-214117 أيضًا مثبطًا محددًا لإشارات البروتينات المكونة للعظام (BMPs) وله تثبيط انتقائي نسبيًا لـ BMP6 بقيمة IC50 تبلغ 100 نانومتريمكن استخدام LDN-214117 لبحوث خلل التنسج الليفي العظمي التدريجي (FOP) والورم الدبقي الجسري الداخلي المنتشر (DIPG)
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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