LDN-214117 是一种口服活性 ALK2 抑制剂，具有良好的耐受性和良好的脑渗透性。 LDN-214117 对 ALK2 具有高选择性和低细胞毒性，IC50 值为 24 nM。 LDN-214117 也是一种特异性骨形态发生蛋白 (BMPs) 信号抑制剂，对 BMP6 具有相对选择性的抑制作用，IC50 值为 100 nM。 LDN-214117可用于进行性骨化性纤维发育不良（FOP）、弥漫性脑桥脑胶质瘤（DIPG）的研究up.
| Cas No. | 1627503-67-6 |
| 化学名 | 1-(4-(6-methyl-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl)phenyl)piperazine |
| Canonical SMILES | CC(C(C1=CC(OC)=C(OC)C(OC)=C1)=C2)=NC=C2C(C=C3)=CC=C3N4CCNCC4 |
| 分子式 | C25H29N3O3 |
| 分子量 | 419.52 |
| 溶解度 | ≥ 90mg/mL in DMSO |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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. |
