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Selleck Chemical LLC SB525334, 1G, potent and selective small-molecule inhibitor of TGFβ receptor I (ALK5), IC50 14.3 nM

Supplier: Selleck Chemical LLC S14761G
SB525334 is a potent and selective small-molecule inhibitor of TGFβ receptor I (ALK5) with an IC50 of 14.3 nM in cell-free assays. It demonstrates high specificity, showing significantly lower potency against ALK4 and no activity against ALK2, ALK3, and ALK6. The compound effectively interferes with TGF-β1-induced phosphorylation and nuclear translocation of Smad2/3, along with suppressing pro-fibrotic gene expression in renal epithelial carcinoma cells. In vivo studies reveal its ability to mitigate renal and pulmonary fibrosis, decrease proteinuria, and impede mesenchymal tumor progression, illustrating its importance for research on TGF-β signaling pathways and related conditions.
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