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Description

A cell-permeable, reversible, substrate competitive inhibitor of protein tyrosine kinases, including autophosphorylation of epidermal growth factor receptor kinase (IC50 = 2.6 µ,M). 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 pp60v-src with similar potencies (IC50 = 20-25 µ,M). Has only a trivial effect on PKC and PKA (IC50 >350 µ,M). 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 µ,M). 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 µ,M). 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.