341216

Ezrin Inhibitor, NSC668394

The Ezrin Inhibitor, NSC668394 controls the biological activity of Ezrin.

• Sinônimo(s): Ezrin Inhibitor, NSC668394, 7-(3,5-dibromo-4-hydroxyphenethylamino)quinoline-5,8-dione
• Fórmula empírica (Notação de Hill): C₁₇H₁₂Br₂N₂O₃
• Número CAS: 382605-72-3
• Peso molecular: 452.10
• Número MDL: MFCD28160708
• Código UNSPSC: 12352200

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥95% (HPLC)
• forma: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: red-orange
• solubilidade: DMSO: 50 mg/mL, clear, red-orange
• Condições de expedição: ambient
• temperatura de armazenamento: −20°C
• cadeia de caracteres SMILES: O=C1C=C(NCCC2=CC(Br)=C(O)C(Br)=C2)C(C3=C1C=CC=N3)=O

Descrição

Descrição geral

A cell-permeable, quinoline that binds directly to ezrin (K_d = 12.6 µM) in a reversible manner, and inhibits PKCι-mediated ezrin phosphorylation at Thr567 (IC₅₀ = 8.1 µM) and ezrin-actin binding, in vitro. It also inhibits murine osteosarcoma K7M2 cell invasion in a monolayer of HUVEC cells, dose-dependently, from 1 to 10 µM. At 10 µM, it causes a unique developmental defect in zebrafish, characterized by reduced motility of eye progenitor cells. Furthermore, this small molecule prevents metastatic growth in an ex vivo mouse lung organ culture assay at 10 µM and attenuates ezrin-dependent OS metastatic growth in mouse lung model in vivo at 2.26 mg/kg/day.

A cell-permeable, quinoline that binds directly to ezrin (K_d = 12.6 µM) in a reversible manner, and inhibits PKCι-mediated ezrin phosphorylation at Thr567 (IC₅₀ = 8.1 µM) and ezrin-actin binding, in vitro. It also inhibits murine osteosarcoma K7M2 cell invasion in a monolayer of HUVEC cells, dose-dependently, from 1 to 10 µM. At 10 µM, it causes a unique developmental defect in zebrafish, characterized by reduced motility of eye progenitor cells. Furthermore, this small molecule prevents metastatic growth in an ex vivo mouse lung organ culture assay at 10 µM and attenuates ezrin-dependent OS metastatic growth in mouse lung model in vivo at 2.26 mg/kg/day.

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Reconstituição

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

Outras notas

Bulut, G., et al. 2011. Oncogene31, 269.

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 2
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable