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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related TGF-β Receptor Products |
|---|
| LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA)
LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. |
| LSKL, Inhibitor of Thrombospondin (TSP-1)
LSKL, Inhibitor of Thrombospondin (TSP-1) is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. |
| KRFK
KRFK, a peptide derived from TSP-1, can activate TGF-β. |
| Maohuoside A
Maohuoside A potently promotes osteogenesis. Maohuoside A enhances the osteogenesis of bone marrow-derived mesenchymal stem cells via bone morphogenetic protein (BMP) and MAPK signaling pathways |
| Vicatertide
Vicatertide is a TGF beta-1 inhibitor. |
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