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Sigma-Aldrich

Rac1 Inhibitor

Rac1 Inhibitor, CAS 1177865-17-6, is a cell-permeable, reversible inhibitor of Rac1 GDP/GTP exchange. Interferes with the interaction between Rac1 and Rac-specific GEFs Trio and Tiam1 (IC₅₀ ~50 µM).

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Synonym(s):
Rac1 Inhibitor, NSC23766
Empirical Formula (Hill Notation):
C24H38Cl3N7
CAS Number:
1177865-17-6
Molecular Weight:
530.96

Quality Level

100

Assay

≥93% (HPLC)

form

lyophilized

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated (hygroscopic)
protect from light

solubility

water: 5 mg/mL

shipped in

ambient

storage temp.

2-8°C

InChI

1S/C24H35N7.3ClH/c1-6-31(7-2)12-8-9-16(3)27-24-28-18(5)14-23(30-24)29-19-10-11-22-20(15-19)21(25)13-17(4)26-22;;;/h10-11,13-16H,6-9,12H2,1-5H3,(H2,25,26)(H2,27,28,29,30);3*1H

InChI key

CPUHORIUXPQCHW-UHFFFAOYSA-N

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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