Tyrosine kinase inhibitor that blocks ERK1/2 phosphorylation
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AG-126

Item No. 13297

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[(3-hydroxy-4-nitrophenyl)methylene]-propanedinitrile
CAS Number
118409-62-4
Synonyms
  • Tyrphostin AG-126
Molecular Formula
C10H5N3O3
Formula Weight
215.2
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 0.15 mg/ml
λmax
210, 305 nm
SMILES
OC1=C([N+]([O-])=O)C=CC(/C=C(C#N)\C#N)=C1
InChi Code
InChI=1S/C10H5N3O3/c11-5-8(6-12)3-7-1-2-9(13(15)16)10(14)4-7/h1-4,14H
InChi Key
DUQADSPERJRQBW-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $31

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    5 mg

    $93

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    10 mg

    $170

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    25 mg

    $347

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    Product 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 vitro and in vivo, attenuating signaling through NF-κB, the induced expression of COX-2 and iNOS, and the inflammatory response in diverse animal models.1,2,3,4,5 AG-126 is a poor inhibitor of epidermal GFRK (IC50 = 450 μM) and platelet-derived GFRK (IC50 > 100 μM).6,7

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    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.K., 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(7), 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(1), 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(5), 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. The Journal of Biological Chemisty 277(39), 36204-36215 (2002).