General description
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 µM). Shown to effectively inhibit Rac1-mediated cellular functions in NIH3T3 and PC-3 cells (effective dose ~50 to 100 μM). 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).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Rac1
Product does not compete with ATP.
Reversible: yes
Target IC50: ~50 µM against Rac1 GDP/GTP exchange activity; 50 mM and 64 mM against TRAP-induced and collagen stimulated platelet aggregation
Packaging
Packaged under inert gas
Warning
Toxicity: Carcinogenic / Teratogenic (D)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Dwivedi, S., et al. 2010. J. Translational Med.8, 128.
Desire, L., et al. 2005. J. Biol. Chem.280, 37516.
Gao, Y., et al. 2004. Proc. Natl. Acad. Sci. USA101, 7618.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 51131638
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 553502-5MG