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.
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.
Embalagem
Packaged under inert gas
Advertência
Toxicity: Standard Handling (A)
Reconstituição
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Outras notas
Bulut, G., et al. 2011. Oncogene31, 269.
Informações legais
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Código de classe de armazenamento
11 - Combustible Solids
Classe de risco de água (WGK)
WGK 2
Ponto de fulgor (°F)
Not applicable
Ponto de fulgor (°C)
Not applicable
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