Rac1 Inhibitor-CAS 1177865-17-6-Calbiochem

C₂₄H₃₈Cl₃N₇

530.96

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
Product does not compete with ATP.
Primary Target
Rac1
Target IC₅₀: ~50 µM against Rac1 GDP/GTP exchange activity; 50 mM and 64 mM against TRAP-induced and collagen stimulated platelet aggregation
Reversible: yes

Toxicity: Carcinogenic / Teratogenic (D)

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

100

≥93% (HPLC)

lyophilized

Calbiochem^®

OK to freeze
desiccated (hygroscopic)
protect from light

water: 5 mg/mL

ambient

2-8℃

10 mg in Glass bottle
5 mg in Plastic ampoule
Packaged under inert gas

11 - Combustible Solids

WGK 3