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Ezrin Inhibitor, NSC668394
7-(3,5-dibromo-4-hydroxyphenethylamino)quinoline-5,8-dione
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.
产品信息
Form Reddish orange solid
Molar mass 449.9
Protect from Light 是的
Packaged under inert gas 是的
Purity ≥95% by HPLC
Solubility DMSO
Chemical formula C17H12Br2N2O3
商店和运输信息
Storage -20°C
Ship Shipped with Blue Ice or with Dry Ice
Standard Handling |