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.

Legal Information

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

Other Notes

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

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

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

Warning

Toxicity: Standard Handling (A)