A cell-permeable, quinoline that binds directly to ezrin (=12.6uM) in a reversible manner, and inhibits PKCι-mediated ezrin phosphorylation at Thr567 (IC50=8.1uM) 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 10uM. At 10uM, 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 10uM and attenuates ezrin-dependent OS metastatic growth in mouse lung model in vitro at 2.26mg/kg/day.
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile ddH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
