SB-431542

SB-431542 is a TGF-β receptor kinase inhibitor (TRKI). SB-431542 has inhibitory activity for ALK4, ALK5 and ALK7 with IC₅₀ values of 1 μM, 0.75 μM and 2 μM, respectively. SB-431542 also inhibits TGF-β-induced transcription, gene expression, apoptosis, and growth suppression. SB-431542 can be used for the research of cancer and signal transduction pathways^[1][2][3]. IC50 & Target:IC50: 1 μM (ALK4); 0.75 μM (ALK5); 2 μM (ALK7)^[1] In Vitro: SB-431542 can inhibit the activity for ALK4, ALK5 and ALK7 with IC₅₀ values of 1 μM, 0.75 μM and 2 μM, respectively^[1].
SB-431542 (0- 10 μM; 24 h) inhibits ALK5 and also the activin type I receptor ALK4 and the nodal type I receptor ALK7, which are very highly related to ALK5 in their kinase domains^[1].
SB-431542 (0.1, 0.5, 1, 5, or 10 μM; 30 min) efficiently inhibits Smad phosphorylation induced by TGF-β and activin but not BMP4^[1].
SB-431542 (0-10 μM) inhibits TGF-beta-induced transcription, gene expression, apoptosis, and growth suppression^[2]. In Vivo: SB-431542 (subconjunctival; 0.5 and 2 mM; on days 1, 2, 3, and 7) inhibits scar formation after glaucoma filtration surgery in New Zealand rabbits^[3].