Description
SB-431542 inhibits activin receptor-like kinases ALK4, ALK5, and ALK7; this inhibition leads to inhibition of activin and TGF-β signaling with no downstream effects on ERK, JNK, or MAPK. SB-431542 exhibits anti-angiogenic and anticancer activity. In vitro, SB-431542 inhibits proliferation and motility of glioma cells. This compound also induces maturation of dendritic cells through its inhibition of TGF-β, increasing IL-12 production and increasing cytotoxic activity of immune cells in vitro.
References
Tanaka H, Shinto O, Yashiro M, et al. Transforming growth factor β signaling inhibitor, SB-431542, induces maturation of dendritic cells and enhances anti-tumor activity. Oncol Rep. 2010 Dec;24(6):1637-43. PMID: 21042762.
Halder SK, Beauchamp RD, Datta PK. A specific inhibitor of TGF-beta receptor kinase, SB-431542, as a potent antitumor agent for human cancers. Neoplasia. 2005 May;7(5):509-21. PMID: 15967103.
Hjelmeland MD, Hjelmeland AB, Sathornsumetee S, et al. SB-431542, a small molecule transforming growth factor-beta-receptor antagonist, inhibits human glioma cell line proliferation and motility. Mol Cancer Ther. 2004 Jun;3(6):737-45. PMID: 15210860.
Inman GJ, Nicolás FJ, Callahan JF, et al. 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. 2002 Jul;62(1):65-74. PMID: 12065756.
