SB 525334

356559-20-1

C21H21N5

DMSO : >= 46 mg/mL (133.95 mM)

TGF-beta/Smad

SB 525334 is a potent and selective transforming growth factor beta1 receptor (ALK5) inhibitor with an IC₅₀ of 14.3 nM. IC50 & Target: IC50: 14.3 nM (ALK5)^[1] In Vitro: SB525334 (1 uM; for 15 minutes before stimulating with 0.625 ng/ml of TGF-beta1, assesses after 6 days) inhibits TGF-beta1-mediated proliferation of familial idiopathic pulmonary arterial hypertension (iPAH) pulmonary artery smooth muscle cells (PASMCs) at an IC₅₀ of 295 nM ^[2]. In Vivo: SB525334 (3-30 mg/kg; p.o.; daily from days 17 to 35) significantly reverses pulmonary arterial pressure in a rat model of pulmonary arterial hypertension (PAH)^[2].