Biochem/physiol Actions

Reversible: yes

Target IC₅₀: 100 nM against epidermal growth factor receptor kinase autophosphorylation

Product does not compete with ATP.

Cell permeable: yes

Primary Targetepidermal growth factor receptor kinase autophosphorylation

General description

A cell-permeable, reversible, substrate competitive, and potent inhibitor of epidermal growth factor receptor kinase autophosphorylation (IC₅₀ = 100 nM). Inhibition of JAK2 by AG 490 selectively blocks leukemic cell growth in vitro and in vivo by inducing programmed cell death, with no harmful effect on normal hematopoiesis. Inhibits the constitutive activation of STAT-3 DNA binding and IL-2-induced growth of MF tumor cells. AG 490 has also been shown to inhibit the autokinase activity of JAK3. A 100 mM (5 mg/170 µl) solution of AG490 (Cat. No. 658411) in DMSO is also available.

A cell-permeable, reversible, substrate competitive, and potent inhibitor of epidermal growth factor receptor kinase autophosphorylation (IC₅₀ = 100 nM). Jak family tyrosine kinase inhibitor. Inhibition of Jak2 by AG 490 selectively blocks leukemic cell growth in vitro and in vivo by inducing programmed cell death, with no harmful effect on normal haematopoiesis. Inhibits the constitutive activation of STAT-3 and IL-2-induced growth of MF tumor cells. AG 490 has also been shown to inhibit the autokinase activity of JAK3. Also reported to inhibit guanylyl cyclase.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Jaleel, M., et al. 2004. Biochemistry43, 8247.Eriksen, K.W., et al. 2001. Leukemia15, 787.Kirken, R.A., et al. 1999. Leukoc. Biol.65, 891.Nielsen, M., et al. 1997. Proc. Natl. Acad. Sci. USA 94, 6764.Meydan, N., et al. 1996. Nature 379, 645.Gazit, A., et al. 1991. J. Med. Chem.34, 1896.Levitzki, A. 1990. Biochem. Pharmacol.40, 913.

Packaging

5 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.

Warning

Toxicity: Standard Handling (A)