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Beschreibung

A cell-permeable, allosteric, trisubstituted dihydropyrazolyl compound that acts as a potent, selective, reversible and non-competitive inhibitor of Cdc42 GTPases (IC50 = 0.2, 2.6 and 5.4 µ,M against nucleotide depleted Cdc42-wt, Cdc42-wt and Cdc42 activated mutant, respectively) with excellent selectivity over Rho family GTPases (IC50 >100 µ,M for Ras-wt, Ras activated mutant, Rab7-wt, Rab2a-wt, Rac1-wt and Rac1 activated mutant). Shown to efficiently block Cdc42 association with GTPgammaS and PAK-PBD, and decrease GTP-Cdc42 (>95%) and GTP-Rac1 (>=40%) contents in EGF-stimulated 3T3 cells, and inhibit Bradykinin (Cat. No. 05-23-0500)-induced filopodia formation in 3T3 cells at 10 µ,M.