中文同义词:
ALK2抑制剂(LDN-214117)
英文同义词:
1-[4-[6-Methyl-5-(3,4,5-trimethoxyphenyl)-3-pyridinyl]phenyl]piperazine;LDN-214117;LDN214117;CS-1539;LDN-214117;1-(4-(6-methyl-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl)phenyl)piperazine;Piperazine, 1-[4-[6-methyl-5-(3,4,5-trimethoxyphenyl)-3-pyridinyl]phenyl]-;LDN-214117 USP/EP/BP
相关类别:
细胞生物学试剂;小分子抑制剂;小分子抑制剂,天然产物;抑制剂;Inhibitors
沸点
567.9±50.0 °C(Predicted)
密度
1.134±0.06 g/cm3(Predicted)
酸度系数(pKa)
8.86±0.10(Predicted)
生物活性
LDN-214117是一种有效的选择性 BMP I型受体激酶 ALK2 抑制剂,IC50为 24 nM。
体外研究
The kinase most highly inhibited by LDN-214117 is ALK2 (IC50, 24 nM), followed by TNIK, RIPK2, and ABL1. LDN-214117 demonstrates selective inhibition of ALK2 and ALK1 in preference to ALK3 kinase activity. LDN-214117 exhibits relatively selective inhibition of BMP6 versus BMP2 or BMP4. In a cell-based assay, LDN-214117 exhibits a selective inhibition on BMP6 with IC50 of approximately 100 nM, and 164-fold selectivity for BMP6 versus TGF-β1.