NSC668394

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NSC668394  纯度: 95.44%

NSC668394 是一种有效的 ezrin (Thr567) 磷酸化抑制剂，Kd 值为 12.59 μM。NSC668394 主要通过与 ezrin 结合来抑制 PKCΙ 导致的 ezrin T567 磷酸化。NSC668394 可用于预防肿瘤转移。

NSC668394

NSC668394 Chemical Structure

CAS No. : 382605-72-3

规格 价格 是否有货 数量
5 mg ￥1200 In-stock
10 mg ￥1800 In-stock
25 mg ￥3700 In-stock
50 mg ￥6000 In-stock
100 mg ￥9800 询价
200 mg   询价  
500 mg   询价  

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NSC668394 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library

生物活性

NSC668394 is a potent ezrin (Thr567) phosphorylation inhibitor, with a Kd 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[1][2][3].

体外研究
(In Vitro)

NSC668394 (10 μM; pretreated for 15 min) inhibits ezrin T567 phosphorylation (IC50=8.1 μM) and actin binding in vitro[1].
NSC668394 (1-10 μM; 2-6 h) inhibits ezrin-mediated invasion by K7M2 osteosarcoma (OS) cells on the HUVEC monolayer[1].
NSC668394 (20 μM) causes significant decrease in growth in JM1 and JM2 rat hepatoma cell lines[2].
NSC668394 (10 μM) reduces cell motility phenotypes in zebrafish[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

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.

体内研究
(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[1].

上海金畔生物科技有限公司 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[1]
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.

分子量

452.10

Formula

C17H12Br2N2O3
CAS 号

382605-72-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 3.85 mg/mL (8.52 mM; ultrasonic and warming and heat to 80°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2119 mL 11.0595 mL 22.1190 mL
5 mM 0.4424 mL 2.2119 mL 4.4238 mL
10 mM — — —

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Bulut G, et, al. Small molecule inhibitors of ezrin inhibit the invasive phenotype of osteosarcoma cells. Oncogene. 2012 Jan 19;31(3):269-81.

    [2]. Xue Y, et, al. Phosphorylated Ezrin (Thr567) Regulates Hippo Pathway and Yes-Associated Protein (Yap) in Liver. Am J Pathol. 2020 Jul;190(7):1427-1437.

    [3]. Çelik H, et, al. Ezrin Inhibition Up-regulates Stress Response Gene Expression. J Biol Chem. 2016 Jun 17;291(25):13257-70.

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