R-268712

879487-87-3

C20H18FN5O

DMSO : 125 mg/mL (343.98 mM; Need ultrasonic)

TGF-beta/Smad

R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM. IC50 value: 2.5 nM [1] Target: ALK5 in vitro: R-268712 is a novel and specific inhibitor of activin receptor-like kinase 5 (ALK5), a transforming growth factor beta (TGF-beta) type I receptor. R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM, an approximately 5000-fold more selectivity for ALK5 than p38 mitogen-activated protein kinase (MAPK). R-268712 is a weak inhibitor of p38 MAP kinase (IC50: 12.1 uM).[1] in vivo: Oral administration of R-268712 at doses of 1, 3 and 10 mg/kg also inhibited the development of renal fibrosis in a dose-dependent manner in a unilateral ureteral obstruction (UUO) model. [1]