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Beschreibung

A cell-permeable pyrimidine compound that specifically and reversibly inhibits Rac1 GDP/GTP exchange activity by interfering with the interaction between Rac1 and Rac-specific GEFs (guanine nucleotide exchange factors) Trio and Tiam1 (IC50 ~50 µ,M). Shown to effectively inhibit Rac1-mediated cellular functions in NIH3T3 and PC-3 cells (effective dose ~50 to 100 muM). Exhibits no effect on Cdc42 or RhoA activation and does not affect Rac1 interaction with BcrGAP or PAK1. Reduces TRAP-induced and collagen stimulated platelet aggregation (IC50 = 50 mM and 64 mM, respectively).