Tyrphostin AG 490

Tyrphostin AG 490

A JAK Inhibitor

Product#:

T-700

Sizes:

10 x 1 mg

5 mg

5 x 5 mg

-490 (AG-490) is synthetic tyrphostin derivated 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). 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

M.W.:

294.31

Structure:

Purity:

>99%

Bioassay:

Tyrphostin AG 490 inhibits the proliferation of Jurkat cells.

Jurkat cells were treated with different concentrations of Tyrphostin AG 490 (#T-700) for four days; the number of live cells were measured by XTT cell proliferation assay kit, normalized to the control (100%) and plotted against drug concentration.

References:

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.

Tyrphostin AG

While many kinase inhibitors are often promiscuous in the enzymes they target, AG-490

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