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。
货号:ajcx35978
CAS:382605-72-3
分子式:C17H12Br2N2O3
分子量：452.1
溶解度:DMSO : 3.85 mg/mL (8.52 mM; ultrasonic and warming and heat to 80°C)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

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].

NSC668394 (0.226 mg/kg/day; i.p. 5-days a week) inhibits ezrin-dependent in vivo OS metastatic growth in mouse lung[1].

[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.