GW788388
TGF-ß receptor kinase inhibitor / 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
Biochemicals & reagents
452342-67-5
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 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 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 Noma et al. (2008), The essential role of fibroblasts in esophageal squamous cell carcinoma-induced angiogenesis; Gastroenterology. 134 1981 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
-20°C
TARGET: Kinase -- PATHWAY: TGF-beta -- RESEARCH AREA: Angiogenesis; Wound healing; Stem cells -- DISEASE AREA: Cancer