Description
Product Usage Information
SB-525334 is supplied as a lyophilized powder. For a 15 mM stock, reconstitute 5 mg of powder in 0.97 mL of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.
Storage
Store lyophilized at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles .
Background
The small-molecule SB-525334 inhibits transforming growth factor-β1 receptor (TGF-βR1, ALK5) with an IC of 14.3 nM. SB-525334 also inhibits the related receptor ALK4 (IC = 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).
Alternate Names
6-[2-(1,1-Dimethylethyl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-4-yl]quinoxaline
