Sigma-Aldrich NSC23766 trihydrochloride. ≥93% (HPLC), lyophilized, Rac1 inhibitor, Calbiochem®. 5 mg

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).

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

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

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.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Carcinogenic / Teratogenic (D)