Genistein; Soybean

Biochem/physiol Actions

Reversible: yes

Primary TargetEGFR kinase

Product does not compete with ATP.

Target IC₅₀: 2.6 µM against autophosphorylation of epidermal growth factor receptor kinase

Cell permeable: yes

General description

A cell-permeable, reversible, substrate competitive inhibitor of protein tyrosine kinases, including autophosphorylation of epidermal growth factor receptor kinase (IC₅₀ = 2.6 µM). The inhibition is competitive with respect to ATP and non-competitive with respect to the phosphate acceptor. Inhibits tumor cell proliferation and induces tumor cell differentiation. Inhibits exogenous substrate phosphorylation by EGFR kinase and pp60^v-src with similar potencies (IC₅₀ = 20-25 µM). Has only a trivial effect on PKC and PKA (IC₅₀ >350 µM). Produces cell cycle arrest and apoptosis in Jurkat T-leukemia cells. Prevents anti-CD3 monoclonal antibody-induced thymic apoptosis. Also inhibits topoisomerase II activity in vitro. Blocks oxidative DNA damage in vitro.

A cell-permeable, reversible, substrate competitive inhibitor of protein tyrosine kinases, including autophosphorylation of epidermal growth factor receptor kinase (IC₅₀ = 2.6 µM). The inhibition is competitive with respect to ATP and non-competitive with respect to the phosphate acceptor. Has only a trivial effect on the activity of PKA and PKC (IC₅₀ >350 µM). Inhibits tumor cell proliferation and induces tumor cell differentiation. Produces cell cycle arrest and apoptosis in Jurkat T-leukemia cells. However, it prevents anti-CD3 monoclonal antibody-induced thymic apoptosis. Also inhibits topoisomerase II activity in vitro.

Legal Information

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

Other Notes

Constantinou, A., and Huberman, E. 1995. Proc. Soc. Exp. Biol. Med. 208, 109.Wei, H., et al. 1995. Proc. Soc. Exp. Biol. Med. 208, 124.Wei, H., et al. 1995. Carcinogenesis17, 73.Kobayashi, S., et al. 1994. J. Biol. Chem.269, 9011.Migita, K., et al. 1994. J. Immunol.153, 3457.Spinozzi, F., et al. 1994. Leuk. Res.18, 431.Dhar, A., et al. 1990. Mol. Pharmacol.37, 519.Hill, T.D., et al. 1990. Science248, 1660.Dean, N.M., et al. 1989. Biochem. Biophys. Res. Commun.165, 795.Akiyama, T., et al. 1987. J. Biol. Chem.262, 5592.

Packaging

50 mg in Plastic ampoule

20 mg in Glass bottle

Warning

Toxicity: Standard Handling (A)