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AG-126

Cayman Chemical Item Number 13297

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

AG-126 (CAS 118409-62-4)

See more	Receptor Biochemistry (344) Inhibitors (546) Cell Biology (303) Inflammation (396) Signal Transduction (328)

Description

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., and 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. Br 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).

Synonyms	Tyrphostin AG-126
Formal Name	2-[(3-hydroxy-4-nitrophenyl)methylene]-propanedinitrile
CAS Number	118409-62-4
Molecular Formula	C₁₀H₅N₃O₃
Formula Weight	215.2
Formulation	A crystalline solid
Purity	≥95%
Stability	2 years
Storage	-20°C
Shipping	Room temperature in continental US; may vary elsewhere
SMILES	Copy SMILES to clipboard OC1=C([N+]([O-])=O)C=CC(/C=C(C#N)\C#N)=C1

Background Reading

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).

Ruetten, H., and 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. Br J Pharmacol 122 59-70 (1997).

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).

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).

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

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

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).

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AG-126 is available in the following screening library:

Bio-active Lipid I Screening Library (96-Well)

Size	Price	Quantity	Subtotal
1 mg	$24.00		$0.00
5 mg	$108.00		$0.00
10 mg	$192.00		$0.00
25 mg	$420.00		$0.00
Bulk	Contact
		Cart Total	$0.00

Pricing updated 2012-05-26. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

Related Products

AG-82

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