GW788388

GW788388 (452342-67-5) is a potent inhibitor of TGF-β receptor kinases ALK4, ALK5 (IC₅₀=18 nM), ALK7, and TGFβRII, but not BMP type II receptor kinase.^1,2 Blocks TGF-β-mediated signaling, including collagen type I and VEGF, in turn reducing fibrosis and angiogenesis in various mouse models.^3,4 GW788388 attenuates TGF-β-induced epithelial to mesenchymal transition (EMT) in human peritoneal mesothelial cells.⁵

References/Citations:

1. Gellibert et al. (2006), Discovery of 4-{4-[3-(pyridine-2-yl)-1H-pyrazol-4-yl}pyridine-2-yl}-N-(tetrahydro-2H-pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor; J. Med. Chem. 49 2210
2. Petersen et al. (2008), Oral administration of GW788388, an inhibitor of TGF-beta type I and II receptor kinases, decreases renal fibrosis; Kidney Int. 73 705
3. De Oliveira et al. (2012), Oral administration of GW788388, an inhibitor of transforming growth factor beta signaling, prevents heart fibrosis in Chagas disease; PLoS Negl. Trop. Dis. 6 e1696
4. Noma et al. (2008), The essential role of fibroblasts in esophageal squamous cell carcinoma-induced angiogenesis; Gastroenterology. 134 1981
5. Lho et al. (2021), Effects of TGF-ß Receptor Inhibitor GW788388 on the Epithelial to Mesenchymal Transition of Peritoneal Mesothelial Cells; Int. J. Mol. Sci. 22 4739