SB431542 is an inhibitor of the transforming growth factor-beta 1 (TGF-β1) activin receptor-like kinases (ALKs). It is a selective and potent inhibitor of ALK-4, -5 and -7. SB431542 inhibits endogenous activin and TGF-β signaling without affecting more divergent BMP signaling utilizing ALK-1, -2, -3, and -61,2. SB431542 stimulates proliferation, differentiation, and sheet formation of endothelial cells derived from embryonic stem cells3.
Matsuyama, S., Iwadate, M., Kondo, M., Saitoh, M., Hanyu, A., Shimizu, K., Aburatani, H., Mishima, H.K., Imamura, T., Miyazono, K., Miyazawa, K. (2003) SB-431542 and Gleevec inhibit transforming growth factor-beta-induced proliferation of human osteosarcoma cells. Cancer Res. 63: 7791-7798.
Laping, N.J., Grygielko, E., Mathur, A., Butter, S., Bomberger, J., Tweed, C., Martin, W., Fornwald, J., Lehr, R., Harling, J., Gaster, L., Callahan, J.F., and Olson, B.A. (2002) Inhibition of transforming growth factor (TGF)-beta1-induced extracellular matrix with a novel inhibitor of the TGF-beta type I receptor kinase activity: SB-431542. Mol Pharmacol 62: 58-64.
Inman, G.J., Nicolás, F.J., Callahan, J.F., Harling, J.D., Gaster, L.M., Reith, A.D., Laping, N.J., and Hill, C.S. (2002) SB-431542 is a potent and specific inhibitor of transforming growth factor-beta superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7. Mol Pharmacol 62: 65-74.
Watabe, T., Nishihara, A., Mishima, K., Yamashita, J., Shimizu, K., Miyazawa, K., Nishikawa, S., and Miyazono, K. (2003) TGF-beta receptor kinase inhibitor enhances growth and integrity of embryonic stem cell-derived endothelial cells. J Cell Biol. 163: 1303-1311.