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:
H2O (5 mg/ml)
Molecular Weight:
~530.96
Storage and Stability:
May be stored at 4 degrees C. For long-term storage, aliquot and store at 4 degrees C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer. This product is sensitive to light.
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