sb525334

SB525334 is a potent and selective small molecule inhibitor of the transforming growth factor-beta receptor I (TGFβRI), also known as activin receptor-like kinase 5 (ALK5). It has an IC50 of 14.3 nM for ALK5 and is about four-fold less potent against ALK4, but inactive against ALK2, ALK3, and ALK6. By inhibiting TGFβRI/ALK5 signaling, SB525334 blocks downstream Smad2/3 phosphorylation and nuclear translocation, reducing expression of genes such as PAI-1 and procollagen α1(I) in renal epithelial carcinoma cells. This inhibition attenuates TGFβ-mediated effects in models of fibrosis and cancer. The compound was initially developed by GlaxoSmithKline for research into fibrotic diseases and cancer[1][4][9].

Other names

6-(2-tert-butyl-5-(6-methylpyridin-2-yl)-1H-imidazol-4-yl)quinoxaline[7]