SB-505124

694433-59-5

C20H21N3O2

DMSO : 113.33 mg/mL (337.90 mM; Need ultrasonic)

TGF-beta/Smad

SB-505124 is a selective inhibitor of TGF-beta Receptor type I receptor (ALK4, ALK5, ALK7), with IC₅₀s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6. IC50 & Target: IC50: 129 nM (ALK4), 47 nM (ALK5) In Vitro: SB-505124 demonstrates no toxicity to renal epithelial A498 cells at concentrations up to 100 uM for 48 h. 505124 inhibits the closely related ALK4 with an IC₅₀ value of 129+/-11 nM (about 2.5-fold less sensitive than ALK5) but does not inhibit ALK2 at concentrations up to 10 uM. SB-505124 (1 uM) inhibits the TGF-beta-induced phosphorylation of Smad2 in all three of these cell lines in a concentration-dependent fashion. SB-505124 (1 or 5 uM) potently inhibits TGF-beta-induced activation of JNK/SAP, extracellular signal-regulated kinase 1/2, and p38 despite the different patterns of activation in these cells^[1]. SB-505124 (10 uM) impairs Smad2 phosphorylation and CTGF and alpha-SMA expression in vitro^[2]. SB-505124 susspresses CTGF and alpha-SMA observed by immunofluorescence. Cell outgrowth from explants dissected from eyes to which SB-505124 is applied during GFS is robust while outgrowth is poor from those treated with MMC^[3].