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. ( Br J Pharmacol. 2005 May;145(2):166-77. ).
CAS 452342-37-9 MFCD52342379
化学结构图
SMILES: c1ccc(-c2cc(-c3c[nH]nc3-c3ccccn3)ccn2)cc1
化学属性
| Mol. Weight | 298.34126 |
|---|---|
| Appearance | Solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name | 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. ( Br J Pharmacol. 2005 May;145(2):166-77. ). |
|---|---|
| Formula | C19H14N4 |
| Synonym | GW6604; GW-6604; GW 6604. |
| IUPAC Name | 2-phenyl-4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridine |
| InChIKey | BDCBRQYHYNUWAM-UHFFFAOYSA-N |
| InChI | InChI=1S/C19H14N4/c1-2-6-14(7-3-1)18-12-15(9-11-21-18)16-13-22-23-19(16)17-8-4-5-10-20-17/h1-13H,(H,22,23) |
| Canonical SMILES | C1(C2=CC=CC=C2)=NC=CC(C3=CNN=C3C4=NC=CC=C4)=C1 |
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- 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. ( Br J Pharmacol. 2005 May;145(2):166-77. ).
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