AG-126

Cayman Chemical Item Number 13297

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

AG-126 (CAS 118409-62-4)

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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
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OC1=C([N+]​([O-]​)​=O)​C=CC(/C=C(C#N)​\C#N)​=C1
InCHI Code
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​1S/C10H5N3O3/c11-5-8(6-12)​3-7-1-2-9(13(15)​16)​10(14)​4-7/h1-4,14H
InCHI Key
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DUQADSPERJRQBW-UHFFFAOYSA-N

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AG-126 is available in the following screening library:

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
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Pricing updated 2014-04-24. Prices are subject to change without notice.

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