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 (IC50~50uM). Shown to effectively inhibit Rac1-mediated cellular functions in NIH3T3 and PC-3 cells (effective dose ~50-100uM). 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 64mM, respectively).Solubility:Soluble to 100mM in water and to 100mM in DMSO.TLC Conditions:Rf = 0.39 (Pyridine: Acetic acid: Water: Butanol [3:8:11:22])Method for Determining Identity:Proton NMR Spectroscopic and Mass Spectrometric AnalysisElemental Analysis:Calculated: %C: 51.66, %H: 7.41, %N: 17.57Storage and Stability:Stored at RT. Stable for 6 months after receipt. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
