Background

In an endeavor to develop novel more potent Rac inhibitors with possible clinical applications, the present invention uses NSC23766 as a lead structure for the design of compounds with 2-3 times enhanced potency.

Thus, the present invention reports the identification and characterization of the biological activity of EHop-016, a novel NSC23766 derivative that inhibits Rac1 100-fold more effectively than the parent compound.

Technology Overview

The compound EHop-016, with an IC50 of 1.1 .mu.M, is a 100-fold more efficient inhibitor of Rac activity than NSC23766. EHop-016 is specific for Rac1 and Rac3 at concentrations .ltoreq.5 mM. At higher concentrations, EHop-016 inhibits the close homolog Cdc42. In MDA-MB-435 cells, EHop-016 (.ltoreq.5mM) inhibits the association of the Rac-GEF Vav2 with a nucleotide-free