5.33982

Dock5 Inhibitor, C21

• Synonym(e): Dock5 Inhibitor, C21, N-(3,5-Dichlorophenyl)benzenesulfonamide
• Empirische Formel (Hill-System): C₁₂H₉Cl₂NO₂S
• CAS-Nummer: 54129-15-6
• Molekulargewicht: 302.18
• MDL number: MFCD01212617
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: powder
• Storage condition: OK to freeze, protect from light

Eigenschaften

• assay: ≥98% (HPLC)
• Quality Segment: 100
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: gray
• solubility: DMSO: 50 mg/mL
• storage temp.: 2-8°C
• SMILES string: [S](=O)(=O)(Nc2cc(cc(c2)Cl)Cl)c1ccccc1
• InChI: 1S/C12H9Cl2NO2S/c13-9-6-10(14)8-11(7-9)15-18(16,17)12-4-2-1-3-5-12/h1-8,15H
• InChI key: HMKZVAZQKOKXRZ-UHFFFAOYSA-N

Beschreibung

General description

A cell-permeable, bioavailable, non-toxic benzenesulfonamide compound that directly blocks Dock5-mediated Rac activation (k_cat/K_M = 7.9 x 10⁴ & 9.5 x 10⁴ M^-1s^-1 for Rac1 & Rac2 by Dock5-DHR2, respectively) with selectivity over RhoA and Cdc42. At higher concentrations, affects Dock1 and Dock2 guanine nucleotide exchange factor activity. Shown to reversibly perturb podosome organization and inhibit osteoclastic bone degradation in a dose-dependent manner. Efficiently prevents both arthritis and metastasis-induced bone loss while preserving bone formation in several osteolytic disease mouse model (25 mg/kg, i.p. or i.v., 5 days a week for 4 weeks). Unlike alendronate (Cat. No. 126855), C21 does not impair bone formation.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
Dock5

Preparation Note

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

Other Notes

Vives, V., et al. 2015. Nat. Commun.6, 6218.
Vives, V., et al. 2011. J. Bone Miner. Res.26, 1099.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Sicherheitshinweise

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