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Cat. No. Name Size Price Add Cart
KI0512AG-49010 mg$80
AG-49025 mg$160

Chemical Characteristic

Product NameAG-490
SynonymsTyrphostin B42
CAS No.133550-30-8
Molecular Weight 294.3
FormulaC17H14N2O3
Chemical Name?(2E)-2-Cyano-3-(3,4-dihydroxyphenyl)-N-(phenylmethyl)-2-propenamide
SmilesC(=O)(/C(=C/c1cc(c(cc1)O)O)/C#N)NCc1ccccc1
Chemical Structure

Biological activities

AG-490 is a specific janus kinase 2 (JAK2) inhibitor. AG-490 inhibits JAK2 with an IC50 of 10 µM.[1] AG-490 blocks the constitutive activation of Stat3sm. AG-490, at concentrations at and above 50 µM, inhibits the spontaneous growth of MF cells with an IC50 of 75 µM. AG-490, at lower concentrations, inhibits the IL-2-mediated up-regulation of MF cell growth with an IC50 of 20 µM. [2] AG-490 potently inhibits the autokinase activity of JAK3 and tyrosine phosphorylation and DNA binding of signal transducer and activator of transcription 5a and 5b (STAT5a/b). AG-490 also inhibits IL-2-mediated proliferative growth in human T cells with an IC50 of 25 µM. AG-490 prevents tetanus toxoid antigen-specific T cell proliferation and expansion. [3] AG-490 inhibits IL-5-induced chemokinesis and β1-integrin adhesiveness of eosinophils in vitro. In vivo, administration of AG-490 prevents antigen-induced eosinophil infiltration in the airways of sensitized mice in a dose-dependent manner. [4] Treatment of mice with AG-490 (dose, 5 mg/kg i.p. simultaneously with zymosan) decreases the number of cells and the level of NO in the peritoneal lavage. Aadministration of AG-490 in zymosan-induced nonseptic shock significantly improves the rate of survival and leads to less exerted signs of multiple organ failure. [5]

Protocols

AG-490 is dissolved in DMSO. [3]

References

[1] Goodman MD, et al. Regulating RISK: a role for JAK-STAT signaling in postconditioning? Am J Physiol Heart Circ Physiol. 2008, 295(4): H1649-1656.
[2] Nielsen M, et al. Constitutive activation of a slowly migrating isoform of Stat3 in mycosis fungoides: tyrphostin AG490 inhibits Stat3 activation and growth of mycosis fungoides tumor cell lines. Proc Natl Acad Sci U S A. 1997, 94(13): 6764-6769.
[3] Kirken RA, et al. Tyrphostin AG-490 inhibits cytokine-mediated JAK3/STAT5a/b signal transduction and cellular proliferation of antigen-activated human T cells. J Leukoc Biol. 1999, 65(6): 891-899.
[4] Kumano K, et al. Blockade of JAK2 by tyrphostin AG-490 inhibits antigen- induced eosinophil recruitment into the mouse airways. Biochem Biophys Res Commun. 2000, 270(1): 209-214.
[5] Dimitrova P, et al. Tyrphostin AG-490 inhibited the acute phase of zymosan-induced inflammation. Int Immunopharmacol. 2008, 8(11): 1567-1577.

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