NSC668394

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

NSC668394 (NSC 668394) 是埃兹蛋白的小分子抑制剂，直接与埃兹蛋白结合，Kd 为 12.59 uM。

NSC668394 (NSC 668394) is a small molecule inhibitor of ezrin, directly bind to ezrin with Kd of 12.59 uM; inhibits T567 phosphorylation and actin binding of endogenous ezrin at 10 μM without altering cellular ezrin levels, inhibits PKC-Ι phosphorylation of recombinant ezrin with IC50 of 8.1 uM; inhibits ezrin-mediated invasion of K7M2 OS cells, inhibits cell motility during zebrafish and Xenopus embryonic development; also inhibits ezrin-dependent in vivo OS metastatic growth in mouse lung.

Western Blot Analysis Cell 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.

Animal Model:Female BALB/c and SCID/Beige mice were injected with K7M2 or MNNG-HOS tumor cellsDosage: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.

NSC 668394 | NSC-668394

Cytoskeleton/Cell Adhesion Molecules

Ezrin

Ezrin

——

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382605-72-3

452.102

C17H12Br2N2O3

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (110.60 mM)

O=C(C=C1NCCC2=CC(Br)=C(O)C(Br)=C2)C3=C(N=CC=C3)C1=O

7-((3,5-dibromo-4-hydroxyphenethyl)amino)quinoline-5,8-dione

(-20℃)

With Ice Pack

≥ 2 years