| Name | GW-6604 |
| Description | GW-6604, an ALK5 inhibitor, exhibits clear antifibrotic effects leading to improved liver function. |
| In vitro | GW-6604 inhibited autophosphorylation of ALK5 with an IC50 of 140 nM and in a cellular assay inhibited TGF-beta-induced transcription of PAI-1 (IC50 = 500 nM)[2]. |
| In vivo | GW-6604 (40 mg/kg p.o.) increased liver regeneration in TGF-beta-overexpressing mice, which had undergone partial hepatectomy. In an acute model of liver disease, GW-6604 reduced by 80% the expression of collagen IA1. In a chronic model of DMN-induced fibrosis where DMN was administered for 6 weeks and GW-6604 dosed for the last 3 weeks (80 mg/kg p.o., b.i.d.), mortality was prevented and DMN-induced elevations of mRNA encoding for collagen IA1, IA2, III, TIMP-1 and TGF-beta were reduced by 50-75%. Inhibition of matrix genes overexpression was accompanied by reduced matrix deposition and reduction in liver function deterioration, as assessed by bilirubin and liver enzyme levels[2]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 2.99 mg/mL (10.02 mM), Sonication is recommended.
|
| Keywords | TGF-β/Smad | TGFβ | TGFbeta/Smad | TGF-beta | TGFbeta | TGF-b/Smad | TGFb | Smad | PAI-1 | PAI1 | GW-6604 | GW6604 | GW 6604 | ALK5 |
| Inhibitors Related | Alectinib | Melamine | SB-431542 | Hydrochlorothiazide | p-Aminobenzamidine dihydrochloride | Crizotinib | Brigatinib | Pirfenidone | A 83-01 | Cetrimonium bromide | Galunisertib | 6-Aminocaproic acid |
| Related Compound Libraries | Anti-Lung Cancer Compound Library | Bioactive Compound Library | Cytokine Inhibitor Library | Membrane Protein-targeted Compound Library | HIF-1 Signaling Pathway Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Inhibitor Library | Metabolism Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | TGF-beta/Smad Compound Library |
United States
