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.

Cell permeable: yes

Primary Target
EGFR kinase

Product does not compete with ATP.

Reversible: yes

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

Toxicity: Standard Handling (A)

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