| Description | NSC668394 is a potent small molecule ezrin (Thr567) phosphorylation inhibitor.NSC668394 has potential antitumor activity by inhibiting ezrin T567 phosphorylation and increasing Ca2+-dependent ezrin cleavage.NSC668394 can be used to study tumor metastasis. |
| In vitro | NSC668394, when pretreated at 10 μM for 15 minutes, inhibits ezrin T567 phosphorylation (IC50=8.1 μM) and in vitro actin binding[2]. Additionally, at concentrations ranging from 1 to 10 μM for 2 to 6 hours, NSC668394 inhibits ezrin-mediated invasion of K7M2 osteosarcoma (OS) cells into HUVEC monolayers[2]. Furthermore, at a concentration of 20 μM, NSC668394 significantly reduces the growth of JM1 and JM2 rat hepatocellular carcinoma cell lines[1].Notably, NSC668394 at 10 μM diminishes cell motility phenotypes in zebrafish[2]. |
| In vivo | 通过每周一次的腹腔注射，连续5天以0.226 mg/kg/日的剂量给药，NSC668394可以抑制小鼠肺部依赖ezrin蛋白的体内转移性生长[2]。 |
| Target activity | Ezrin T567:8.1 μM |
| Synonyms | NSC-668394, NSC 668394 |
| molecular weight | 452.1 |
| Molecular formula | C17H12Br2N2O3 |
| CAS | 382605-72-3 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 30 mg/mL(66.36 mM), Sonication is recommended. |
| References | 1. 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. 2. Bulut G, et, al. Small molecule inhibitors of ezrin inhibit the invasive phenotype of osteosarcoma cells. Oncogene. 2012 Jan 19;31(3):269-81. 3. Çelik H, et, al. Ezrin Inhibition Up-regulates Stress Response Gene Expression. J Biol Chem. 2016 Jun 17;291(25):13257-70. |