GW-6604
| CAS号 | 452342-37-9 | 货号 | BCP13570 |
| 中文名 | GW-6604 | ||
| 英文名 | GW-6604 | ||
| 中文别名 | |||
| 英文别名 | GW6604;GW 6604; | ||
| 分子式 | C19H14N4 | 分子量 | 298.35 |
| 生物活性 | GW6604 is a potent and selective ALK-5 inhibitor with potent anticancer activity. GW6604 is also a TGF-beta signaling pathway inhibitor. In vitro, GW6604 inhibited autophosphorylation of ALK5 with an IC(50) of 140 nM and in a cellular assay inhibited TGF-beta-induced transcription of PAI-1 (IC(50): 500 nM). In vivo, GW6604 (40 mg kg(-1) p.o.) increased liver regeneration in TGF-beta-overexpressing mice, which had undergone partial hepatectomy. In an acute model of liver disease, GW6604 reduced by 80% the expression of collagen IA1. Inhibition of ALK5 could be an attractive new approach to treatment of liver fibrotic diseases by both preventing matrix deposition and promoting hepatocyte regeneration. | ||
| 信号通路 | Angiogenesis/Protein Tyrosine Kinase | ||
| 靶 点 | ALK | ||
结构式
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