553502

NSC23766 trihydrochloride

≥93% (HPLC), lyophilized, Rac1 inhibitor, Calbiochem^®

• Synonym(s): Rac1 Inhibitor, NSC23766
• Empirical Formula (Hill Notation): C₂₄H₃₈Cl₃N₇
• CAS Number: 1177865-17-6
• Molecular Weight: 530.96
• MDL number: MFCD08703096
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥93% (HPLC)
• Form: lyophilized
• Storage condition: OK to freeze, desiccated (hygroscopic), protect from light

Properties

• Product Name: 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).
• Quality Segment: 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
• SMILES string: Cl.Cl.Cl.N(CCCC(Nc1nc(cc(n1)C)Nc2cc3c(nc(cc3N)C)cc2)C)(CC)CC
• 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

Description

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

Preparation Note

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

Disclaimer

Toxicity: Carcinogenic / Teratogenic (D)

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable