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341216 Sigma-Aldrich

Ezrin Inhibitor, NSC668394 - Calbiochem

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

Synonym: 7-(3,5-dibromo-4-hydroxyphenethylamino)quinoline-5,8-dione, Ezrin Inhibitor, NSC668394 - Calbiochem

  • Empirical Formula (Hill Notation) C17H12Br2N2O3

  • Molecular Weight 452.10

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Properties

Quality Level   100
assay   ≥95% (HPLC)
form   solid
mfr. no.   Calbiochem®
storage condition   OK to freeze
  protect from light
storage conditions   -20C
color   red-orange
solubility   DMSO: 50 mg/mL, clear, red-orange
shipped in   ambient

Description

General description

A cell-permeable, quinoline that binds directly to ezrin (Kd = 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

10 mg in Glass bottle

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.

Safety & Documentation

Safety Information

Safety Information for this product is unavailable at this time.
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