Background:

SB505124 is a selective and small molecule inhibitor of transforming growth Factor- β type 1 receptors ALK4, ALK5 and ALK7 with the IC50 values of 129±11nM and 47±5nM for ALK4 and ALK5, respectively. [1].

SB505124 has been reported as a potent inhibitor of the in vitro kinase activity of ALK4, ALK5 and ALK7 for its substrate Smad3. In addition, SB505124 has been revealed to be a reversible ATP competitive inhibitor. Moreover, SB505124 has shown no toxicity to renal epithelial A498 cells at concentrations up to 100μM for 48 h. Furthermore, SB505124 has been demonstrated to restrain the TGF-β-induced phosphorylation of Smad2 in three cell lines (HepG2 human hepatoma cells, C2C12 mouse myoblasts and Mv1Lu mink lung cells) in a concentration-dependent manner [1].

参考文献:
[1] DaCosta Byfield S1, Major C, Laping NJ, Roberts AB. SB-505124 is a selective inhibitor of transforming growth factor-beta type I receptors ALK4, ALK5, and ALK7. Mol Pharmacol. 2004 Mar;65(3):744-52.