341216

Ezrin Inhibitor, NSC668394

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

• Synonym(s): Ezrin Inhibitor, NSC668394, 7-(3,5-dibromo-4-hydroxyphenethylamino)quinoline-5,8-dione
• Empirical Formula (Hill Notation): C₁₇H₁₂Br₂N₂O₃
• CAS Number: 382605-72-3
• Molecular Weight: 452.10
• MDL number: MFCD28160708
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: red-orange
• solubility: DMSO: 50 mg/mL, clear, red-orange
• shipped in: ambient
• storage temp.: −20°C
• SMILES string: O=C1C=C(NCCC2=CC(Br)=C(O)C(Br)=C2)C(C3=C1C=CC=N3)=O

Description

General description

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.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 2
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable