SB-525334

• GMP format available

SB-525334 is a potent inhibitor of the transforming growth factor β1 receptor (ALK5). It has an IC50 of 14.3 nM for ALK5.

Key features and applications include:

• High Selectivity: Specifically inhibits ALK5 with minimal activity against other ALK receptors.
• Potency: Demonstrates strong inhibitory effects with an IC50 of 14.3 nM.
• Block Phosphorylation and Nuclear Translocation of Smad2/3: This inhibition reduces PAI-1 and procollagen α1 (I) mRNA expression in renal epithelial carcinoma cells.
• Reduce Fibrosis: Effective in models of pulmonary fibrosis and renal disease by decreasing TGF-β-mediated responses.
• Attenuate Pulmonary Arterial Hypertension: Lowers pulmonary arterial pressure and right ventricular hypertrophy in relevant models.

Relevant disease states include:

• Pulmonary Fibrosis: Reduces myofibroblast proliferation and fibrosis.
• Renal Disease: Decreases markers of fibrosis in renal epithelial carcinoma cells.
• Pulmonary Arterial Hypertension: Mitigates symptoms by reducing TGF-β sensitivity.