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

452342-37-9
SMILES: c1ccc(-c2cc(-c3c[nH]nc3-c3ccccn3)ccn2)cc1

化学属性

Mol. Weight298.34126
Appearance Solid powder
SolubilitySoluble in DMSO, not in water

别名和识别编码

Chemical NameGW6604 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. ).
FormulaC19H14N4
Synonym GW6604; GW-6604; GW 6604.
IUPAC Name2-phenyl-4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridine
InChIKeyBDCBRQYHYNUWAM-UHFFFAOYSA-N
InChIInChI=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 SMILESC1(C2=CC=CC=C2)=NC=CC(C3=CNN=C3C4=NC=CC=C4)=C1
信息真实价格透明    资金保障    专业采购外包团队在线服务   
信息真实价格透明    资金保障    专业采购外包团队在线服务   
品牌质保精细包装    现货库存    一流品牌服务   

产品应用

  • 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. ).

安全信息

Storage condition Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

系列性分类


相关产品推荐