NSC668394

NSC668394 is a potent ezrin (Thr567) phosphorylation inhibitor, with a K d of 12.59 μM. NSC668394 inhibit ezrin T567 phosphorylation caused by PKCΙ primarily via their binding to ezrin. NSC668394 can be used to prevent tumor metastasis . In Vitro NSC668394 (10 μM; pretreated for 15 min) inhibits ezrin T567 phosphorylation (IC 50 =8.1 μM) and actin binding in vitro. NSC668394 (1-10 μM; 2-6 h) inhibits ezrin-mediated invasion by K7M2 osteosarcoma (OS) cells on the HUVEC monolayer. NSC668394 (20 μM) causes significant decrease in growth in JM1 and JM2 rat hepatoma cell lines. NSC668394 (10 μM) reduces cell motility phenotypes in zebrafish. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: K7M2 OS cells Concentration: 10 μM Incubation Time: 6 hours Result: Inhibited T567 phosphorylation and actin binding of endogenous ezrin without altering cellular ezrin levels. In Vivo NSC668394 (0.226 mg/kg/day; i.p. 5-days a week) inhibits ezrin-dependent in vivo OS metastatic growth in mouse lung . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female BALB/c and SCID/Beige mice were injected with K7M2 or MNNG-HOS tumor cells Dosage: 0.226 mg/kg/day Administration: I.p. 5-days a week for 66 days Result: Showed an increase in survival. Decreased the number of the green fluorescent protein (GFP)-expressing metastatic foci in the lung tissues. Form:Solid

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