SB-525334 #20090
Product Information
Product Usage Information
Storage
Product Description
| Molecular Weight | 343.4 g/mol |
| Purity | >99% |
| Molecular Formula | C21H21N5 |
| CAS | 356559-20-1 |
| Solubility | Soluble in DMSO at 30 mg/mL. |
Background
The small-molecule SB-525334 inhibits transforming growth factor-β1 receptor (TGF-βR1, ALK5) with an IC50 of 14.3 nM. SB-525334 also inhibits the related receptor ALK4 (IC50 = 58.5 nM) but is inactive against ALK2, ALK3, and ALK6. Inhibition of TGF-β downstream signaling by SB-525334 blocks phosphorylation and nuclear translocation of Smad2/3 protein and reduces PAI-1 and procollagen α1(I) mRNA expression in renal epithelial carcinoma cells (1). SB-525334 treatment of a bleomycin-induced pulmonary fibrosis model reduced TGF-β-mediated nuclear translocation of Smad2/3, decreased myofibroblast proliferation, and attenuated pulmonary fibrosis (2). Exposure of mesenchymal and epithelial tumors in Eker rats to SB-525334 reduced the size and number of mesenchymal tumors but had the opposite effect on epithelial cancer cells and lesions (3). Inhibition of ALK5 by SB-525334 in both human pulmonary artery smooth muscle cells and a rat model of pulmonary arterial hypertension resulted in decreased sensitivity to TGF-β, and attenuated pulmonary arterial pressure and right ventricular hypertrophy (4).
Limited Uses
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