4′,5,7-Trihydroxyisoflavone Pale yellow solid. PROTECT FROM LIGHT. Inhibits 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. Purity: ≥95% by HPLC. RTECS NR2392000, CAS 446-72-0. Merck Index: 14, 4391
Ref.: 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. Carcinogenesis 17, 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. Science 248, 1660. Dean, N.M., et al. 1989. Biochem. Biophys. Res. Commun. 165, 795. Akiyama, T., et al. 1987. J. Biol. Chem. 262, 5592. |
