sb525334

Description: SB525334 (SB-525334; SB 525334) is a potent and selective inhibitor of TGF-beta (transforming growth factor-beta) receptor I, ALK5 (activin receptor-like kinase) with potential anti-fibrotic activity. It inhibits TGF-beta with an IC50 of 14.3 nM in a cell-free assay. SB525334 is 4-fold less potent to ALK4 than ALK5 and is inactive against ALK2, 3, and 6. In cell-based assays, SB-525334 at the concentration of 1 uM 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.

References: J Pharmacol Exp Ther. 2005 Jun; 313(3):943-51; Am J Pathol. 2009 Feb; 174(2):380-9.

SB 525334; SB-525334; SB525334

Chemical Name: 6-(2-(tert-butyl)-5-(6-methylpyridin-2-yl)-1H-imidazol-4-yl)quinoxaline

SMILES Code: CC1=CC=CC(C2=C(C3=CC=C4N=CC=NC4=C3)N=C(C(C)(C)C)N2)=N1

Exact Mass: 343.1797