Cayman Chemical | AG-126 | Description • Tyrphostin AG-126 (CAS 118409-62-4)

13297 AG-126

Tyrphostin AG-126 (CAS 118409-62-4)

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• See more Inhibitors; Cell Biology; Inflammation; Signal Transduction

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Tyrphostins are a family of protein tyrosine kinase inhibitors originally developed to inhibit cell growth by blocking the activity of certain growth factor receptor kinases (GFRK). The tyrphostin AG-126 selectively inhibits the phosphorylation of ERK1 (p44) and ERK2 (p42) at 25-50 μM.^1,2 It blocks the production of TNF-α in vitro² and in vivo,¹ attenuating signaling through NF-κB,¹ the induced expression of COX-2 and iNOS,^3,4 and the inflammatory response in diverse animal models.^3,5 AG-126 is a poor inhibitor of epidermal GFRK (IC₅₀ = 450 μM)⁶ and platelet-derived GFRK (IC₅₀ > 100 μM).⁷

1 Novogrodsky, A., Vanichkin, A., Patya, M., et al. Prevention of lipopolysaccharide-induced lethal toxicity by tyrosine kinase inhibitors. Science 264(5163) 1319-1322 (1994).

2 Hanisch, U., Prinz, M., Angstwurm, K., et al. The protein tyrosine kinase inhibitor AG126 prevents the massive microglial cytokine induction by pneumococcal cell walls. Eur J Immunol 31 2104-2115 (2001).

3 Cuzzocrea, S., McDonald, M.C., Mazzon, E., et al. The tyrosine kinase inhibitor tyrphostin AG126 reduces the development of acute and chronic inflammation. Am J Pathol 157(1) 145-158 (2000).

4 Ruetten, H., Thiemermann, C. Effects of tyrphostins and genistein on the circulatory failure and organ dysfunction caused by endotoxin in the rat: A possible role for protein tyrosine kinase. Brit J Pharmacol 122 59-70 (1997).

5 Chatterjee, P.K., Patel, N.S.A., Kvale, E.O., et al. The tyrosine kinase inhibitor tyrphostin AG126 reduces renal ischemia/reperfusion injury in the rat. Kidney Int 64 1605-1619 (2003).

6 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).

7 Sagara, Y., Ishige, K., Tsai, C., et al. Tyrphostins protect neuronal cells from oxidative stress. J Biol Chem 277(39) 36204-36215 (2002).

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Pricing updated 2010-03-13.
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Stability of this item is suitable for room temperature overnight shipping. If shipment on ice is desired, it must be requested when the order is placed.