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GW788388 is a selective inhibitor of transforming growth factor-β type I receptor (ALK5) (IC50 values are 0.018 and 0.093 μM for ALK5 binding and for TGF-β cellular assay respectively). GW788388 inhibits esophageal squamous cell carcinoma (ESCC)-induced neoangiogenesis. GW788388 is orally available with a half-life of approximately 4 hours. GW788388 blocked TGF-beta-induced Smad activation and target gene expression, while decreasing epithelial-mesenchymal transitions and fibrogenesis. Treatment with GW788388 significantly reduced TGF-beta activity, leading to the attenuation of systolic dysfunction and left ventricular remodeling in an experimental rat model of MI.
| Molecular Weight | 425.48 |
| Formula | C25H23N5O2 |
| CAS Number | 452342-67-5 |
| Solubility (25°C) | DMSO 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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