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SB-525334 is a potent and selective inhibitor of the transforming growth factor-beta1 (TGF-beta1) receptor, activin receptor-like kinase (ALK5). In cell-based assays, SB-525334 (1 microM) blocked TGF-beta1-induced phosphorylation and nuclear translocation of Smad2/3 in renal proximal tubule cells and inhibited TGF-beta1-induced increases in plasminogen activator inhibitor-1 (PAI-1) and procollagen alpha1(I) mRNA expression in A498 renal epithelial carcinoma cells. SB-525334 inhibited ALK5 kinase activity with an IC50 of 14.3 nM and was approximately 4-fold less potent as an inhibitor of ALK4 with IC50 of 58.5 nM. SB-525334 significantly increased apoptotic cell death in gemcitabine-resistant cells. SB-525334 reverses pulmonary arterial pressure and inhibits right ventricular hypertrophy in a rat model of PAH effectively. SB-525334 treatment showed significant attenuation in Smad2/3 nuclear translocation, decrease in CTGF-expressing cells, myofibroblast proliferation and type I collagen deposition.
Cancer Biother Radiopharm. 2020 Mar;35(2):120-128.
Activation of TGF-β1 Pathway by SCUBE3 Regulates TWIST1 Expression and Promotes Breast Cancer Progression.
SB-525334 purchased from AbMole
J Cell Physiol. 2019 Jun;234(6):9698-9710.
H19/miR-148a/USP4 axis facilitates liver fibrosis by enhancing TGF-β signaling in both hepatic stellate cells and hepatocytes.
SB-525334 purchased from AbMole
Oncol Lett. 2018 Dec 10.
Pancreatic stellate cells facilitate pancreatic cancer cell viability and invasion.
SB-525334 purchased from AbMole
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Source | Am J Physiol Renal Physiol (2015). Figure 4. SB-525334 |
| Method | Endothelial function | |
| Cell Lines | rats | |
| Concentrations | - | |
| Incubation Time | 24-h | |
| Results | Aortic endothelial cell lysates obtained from the four groups of rats on day 7 of the experiment demonstrated activation of ALK5 by HS intake as well as the anticipated inhibition of ALK5 by SB-525334 |
| Molecular Weight | 343.42 |
| Formula | C21H21N5 |
| CAS Number | 356559-20-1 |
| Solubility (25°C) | DMSO 60 mg/mL Ethanol 40 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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