AG-112

AG-112 is an EGFR inhibitor.¹ It inhibits EGFR-catalyzed phosphorylation of poly(GAT) in a cell-free assay (IC₅₀ = 0.125 µM). AG-112 also inhibits calcineurin phosphatase activity in a cell-free assay (IC₅₀ = 30 µM).² AG-112 inhibits diabetes-induced growth of vascular smooth muscle cells (VSMCs) isolated from type 2 diabetic rats and reduces diabetes-induced increases in superoxide generation and NADPH oxidase activity in the same cells.³

WARNING This product is not for human or veterinary use.

1. Gazit, A., Yaish, P., Gilon, C., et al. Tyrphostins I: Synthesis and biological activity of protein tyrosine kinase inhibitors. J. Med. Chem. 32(10), 2344-2352 (1989).

2. Martin, B.L. Inhibition of calcineurin by the tyrphostin class of tyrosine kinase inhibitors. Biochem. Pharmacol. 56(4), 483-488 (1998).

3. Jeong, H.Y., Son, S.M., Kim, Y.K., et al. Tyrosine kinase-mediated activation of NADPH oxidase enhances proliferative capacity of diabetic vascular smooth muscle cells. Life Sci. 76(15), 1747-1757 (2005).