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ALK-5 inhibitor GW6604

ALK-5 inhibitor GW6604 452342-37-9
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Chemical Information
Product name:ALK-5 inhibitor GW6604 Purity:98% min
CAS NO:452342-37-9 Solubility:Soluble in DMSO
Molecular Formula:C19H14N4 Package:Package according to customer requirements
Molecular Weight:298.341 Storage:Store at -20℃
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Remarks
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.
References

1: Ciayadi R, Kelso GF, Potdar MK, Harris SJ, Walton KL, Harrison CA, Hearn MT. Identification of protein binding partners of ALK-5 kinase inhibitors. Bioorg Med Chem. 2013 Nov 1;21(21):6496-500. doi: 10.1016/j.bmc.2013.08.038. Epub 2013 Aug 29. PubMed PMID: 24055074.

2: de Gouville AC, Huet S. Inhibition of ALK5 as a new approach to treat liver fibrotic diseases. Drug News Perspect. 2006 Mar;19(2):85-90. Review. PubMed PMID: 16628263.

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