AG-556

AG-556 is a tyrphostin inhibitor of EGFR (IC₅₀ = 5 µM).¹ It is selective for EGFR over HER2 (IC₅₀ = >500 µM). AG-556 inhibits EGF-induced growth of HER14 cells (IC₅₀ = 3 µM). It inhibits hydrogen peroxide-induced increases in intracellular calcium in HEK293 cells expressing human transient receptor potential melastatin 2 (TRPM2; IC₅₀ = 0.94 µM), as well as HEK293 cells expressing human TRP ankyrin 1 (TRPA1) when used at a concentration of 3 µM.² AG-556 (200 µg/animal per day) reduces the incidence, severity, and duration of disease in a mouse model of experimental autoimmune encephalomyelitis (EAE).³ It reduces edema, demyelination, and myeloperoxidase (MPO) activity, a marker of neutrophil infiltration, in spinal cord tissue, as well as improves motor function in a mouse model of extradural compression-induced spinal cord injury when administered at a dose of 10 mg/kg.⁴

WARNING This product is not for human or veterinary use.

1. Gazit, A., Osherov, N., Posner, I., et al. Tyrphostins. 2. Heterocyclic and α-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases. J. Med. Chem. 34(6), 1896-1907 (1991).

2. Toda, T., Yamamoto, S., Yonezawa, R., et al. Inhibitory effects of Tyrphostin AG-related compounds on oxidative stress-sensitive transient receptor potential channel activation. Eur. J. Pharmacol. 786, 19-28 (2016).

3. Brenner, T., Poradosu, E., Soffer, D., et al. Suppression of experimental autoimmune encephalomyelitis by tyrphostin AG-556. Exp. Neurol. 154(2), 489-498 (1998).

4. Genovese, T., Mazzon, E., Esposito, E., et al. Inhibition of tyrosine kinase-mediated cellular signalling by Tyrphostins AG126 and AG556 modulates secondary damage in experimental spinal cord trauma. Neuropharmacology 52(7), 1454-1471 (2007).