AG-9

AG-9 is an immunomodulatory agent.^1,2 It selectively inhibits IL-12-induced tyrosine phosphorylation of TYK2 and STAT3 over JAK2 in primary mouse T cells activated by concanavalin A (Item No. 14951) when used at a concentration of 10 µM.¹ Unlike most tyrphostins, it does not inhibit EGFR (IC₅₀ = >1,250 µM) and has commonly been used as an inactive control for tyrphostin tyrosine kinase inhibitory activity.^3,2 AG-9 inhibits IL-12 production and NF-κB translocation induced by CD40 ligand (CD40L) in primary mouse macrophages and reduces the development and severity of experimental autoimmune encephalomyelitis (EAE) in mice.² It also inhibits GABA-induced activation of wild-type GABA_A receptors and GABA_A receptors containing tyrosine-to-phenylalanine mutations at positions 365 and 367 expressed in Xenopus oocytes when used at a concentration of 200 µM.⁴

WARNING This product is not for human or veterinary use.

1. Bright, J.J., Du, C., and Sriram, S. Tyrphostin B42 inhibits IL-12-induced tyrosine phosphorylation and activation of Janus kinase-2 and prevents experimental allergic encephalomyelitis. J. Immunol. 162(10), 6255-6262 (1999).

2. Du, C., Bright, J.J., and Sriram, S. Inhibition of CD40 signaling pathway by tyrphostin A₁ reduces secretion of IL-12 in macrophage, Th1 cell development and experimental allergic encephalomyelitis in SJL/J mice. J. Neuroimmunol. 114(1-2), 69-79 (2001).

3. 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).

4. Dunne, E.L., Moss, S.J., and Smart, T.G. Inhibition of GABA_A receptor function by tyrosine kinase inhibitors and their inactive analogues. Mol. Cell. Neurosci. 12(4-5), 300-310 (1998).