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-Nummer: MFCD01212617
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Assay: ≥98% (HPLC)
• Qualitätsniveau: 100
• Form: powder
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: gray
• Löslichkeit: DMSO: 50 mg/mL
• Lagertemp.: 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
• InChIKey: HMKZVAZQKOKXRZ-UHFFFAOYSA-N

Beschreibung

Allgemeine Beschreibung

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. Wirkung

Cell permeable: yes

Primary Target
Dock5

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

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

Sonstige Hinweise

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

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable