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SB-505124 is a selective inhibitor of transforming growth factor-β type I receptor (ALK5), ALK4 and ALK7 (IC50 values are 47 and 129 nM for ALK5 and ALK4 respectively). SB-505124 also blocks more complex endpoints of TGF-beta action, as evidenced by its ability to abrogate cell death caused by TGF-beta1 treatment. SB-505124 is three to five times more potent than a related ALK5 inhibitor described previously, SB-431542.
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Source | Arthritis Res Ther (2017). Figure 1. SB-505124 |
| Method | Western Blot | |
| Cell Lines | Primary bovine chondrocytes | |
| Concentrations | 5 μM | |
| Incubation Time | 1 h | |
| Results | Subsequently, we analyzed the effects of the ALK4/5/7-kinase inhibitor SB-505124, the ALK1/2/3-kinase inhibitor LDN-193189 and the TAK1-kinase inhibitor (5Z)-7-Oxozeaenol on TGFβ1-induced R-Smad phosphorylation |
| Molecular Weight | 335.4 |
| Formula | C20H21N3O2 |
| CAS Number | 694433-59-5 |
| Solubility (25°C) | DMSO 90 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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