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Tyrphostin AG 490

A JAK Inhibitor

Cat #: T-700
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 294.31
    Purity: >99%
    Effective concentration 10 nM - 1 µM.
    Structure
    Chemical name (E)-2-Cyano-3-(3,4-dihydrophenyl)-N-(phenylmethyl)-2-propenamide.
    Molecular formula C17H14N2O3.
    CAS No.: 134036-52-5
    Activity Tyrphostin AG 490 is a potent inhibitor of JAK2 and JAK3. In addition, Tyrphostin AG 490 inhibits the JAK3/STAT, JAK3/AP-1, and JAK3/MAPK pathways and their cellular consequences1.
    References-Activity
    1. Wang, L.H. et al. (1999) J. Immunol162, 3897.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to two weeks at 4°C or six months at -20°C.
    Our bioassay
    • Alomone Labs Tyrphostin AG 490 inhibits the proliferation of Jurkat cells.
      Alomone Labs Tyrphostin AG 490 inhibits the proliferation of Jurkat cells.
      Cells were treated with different concentrations of Tyrphostin AG 490 (#T-700) for 4 days. Cell survival was measured after 4 days using the XTT method, calculated as a relative percentage of the control without Tyrphostin AG 490 and plotted against drug concentrations.
    References - Scientific background
    1. Gazit, A. et al. (1989) J. Med. Chem. 32, 2344.
    2. Levitzki, A. and Gazit, A. (1995) Science 267, 1782.
    3. Wang, L.H. et al. (1999) J. Immunol. 162, 3897.
    4. Kirken, R.A. et al. (1999) J. Leukocyte Biol. 65, 891.
    5. Meydan, N. et al. (1996) Nature 379, 645.
    6. Simon, H. U. et al. (1997) Eur. J. Immunol. 27, 3536.
    7. Marrero, M.B. et al. (1997) J. Biol. Chem. 272, 24684.
    8. McWhinney, C.D. et al. (1997) J. Mol. Cell. Cardiol. 29, 2513.
    9. Nielsen, M. et al. (1997) Proc. Natl. Acad. Sci. USA 94, 6764.
    10. Bacon, C.M. et al. (1995) Proc. Natl. Acad. Sci. USA 92, 7307.
    11. De Vos, J. et al. (2000) Br. J. Haematol. 109, 823.
    Scientific background

    Tyrphostin AG-490 (AG-490) is synthetic tyrphostin derived from benzylidine malononitrile.1 At relatively low concentrations, AG-490 was found to be a highly efficient tyrosine kinase inhibitor for hyperactive forms of Jun kinase 2, 3 and 5 (Jak 2,3, and 5).

    While many kinase inhibitors are often promiscuous in the enzymes they target, AG-490 is unique in that it does not inhibit other lymphocytic tyrosine kinases such as Lck, Lyn, Btk, Syk, Src, Jak1, Zap70 or Tyk2. 2-6 AG-490 has also been shown to inhibit cytokine-induced activation of JAK2 in eosinophils stimulated with granulocyte-macrophage and in vascular smooth muscle cells and cardiac myocytes activated by angiotensin II. 7-9

    Some studies have demonstrated that AG-490 efficiently blocks STAT3 activation in mycosis fungoides-derived T cell lymphoma cells and induces apoptosis in myeloma cells.10-11

    Last update: 13/10/2022

    Tyrphostin AG 490 (#T-700) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use

    Applications

    Specifications

    Scientific Background

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