A cell-permeable trisubstituted dihydropyrazolyl compound that acts as a potent, selective, reversible and non-competitive inhibitor of Cdc42 GTPases (IC50=0.2, 2.6 and 5.4uM against nucleotide depleted Cdc42-wt, Cdc42-wt and Cdc42 activated mutant, respectively) with excellent selectivity over Rho family GTPases (IC50>100uM for Ras-wt, Ras activated mutant, Rab7-wt, Rab2a-wt, Rac1-wt and Rac1 activated mutant). Shown to efficiently block Cdc42 association with GTPyS and PAK-PBD, and decrease GTP-Cdc42 (>95%) and GTP-Rac1 (>40%) contents in EGF-stimulated 3T3 cells, and inhibit Bradykinin-induced filopodia formation in 3T3 cells at 10uM.
Formula:C22H21N3O3S
Solubility:DMSO
Molecular Weight:407.5
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
