ML347 是一种选择性的 ALK1/ALK2 抑制剂,它们的 IC50 分别为 46/32 nM,比对 ALK3 的抑制性高 300 倍。
产品描述
ML347(DN193719) is a highly specific ALK1/2 inhibitor ( IC50: 46/32 nM), and the selectivity for ALK2 is >300-fold than ALK3.
体内活性
在人类和大鼠血浆中,ML347与血浆蛋白的结合力较高。ML347在BMP应答的C2C12BRA细胞中也有一定效能(IC50:15 nM)。
激酶实验
Kinase assay: All kinase assays are conducted by Reaction Biology Corp. In brief, compounds are tested at 10 concentrations by 3-fold serial dilutions starting at 30 μM, using nonspecific kinase inhibitor staurosporine as control. In vitro kinase reactions are carried out in the presence of 10 μM (33P)γATP. Five kinases tested are the human BMP type-I receptor activin receptor-like kinase 2 (ALK-2/ACVR1), the human TGFβ type-I receptor activin receptor-like kinase 5 (Alk5/TGFβR1), the human VEGF type-II receptor (KDR/Flk-1/VEGFR2), the human AMP-activated protein kinase (AMPK/A1/B1/G1) and the human platelet-derived growth factor receptor-β (PDGFRβ).
Cas No.
1062368-49-3
分子式
C22H16N4O
分子量
352.39
别名
LDN 193719
储存和溶解度
DMSO:7.1 mg/mL (20 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years