| Bioactivity | Sepin-1 is a potent separase inhibitor with an IC50 value of 14.8 µM. Sepin-1 inhibits cell proliferation, migration and wound healing. Sepin-1 decreases the expression of FoxM1 protein and mRNA level. Sepin-1 shows anti-tumor activity[1][2]. | ||||||||||||
| Target | IC50: 14.8 µM (separase) | ||||||||||||
| Invitro | Sepin-1 (0, 20, 40 µM; 24 h) 抑制细胞迁移和伤口愈合，并引起 DNA 损伤[1]。Sepin-1 (0, 10, 20, 40 µM; 24 h) 以剂量依赖性方式降低 FoxM1 蛋白和 mRNA 水平的表达[1]。Sepin-1 (0, 10, 20, 40 µM; 24 h) 抑制 Plk1、Cdk1、pericentrin、Aurora 和 Lamin B1 蛋白水平的表达[1]。 Cell Proliferation Assay[1] Cell Line: | ||||||||||||
| In Vivo | Sepin-1 (10 mg/kg；静脉注射；每天一次，每周 5 天，持续 3 周) 在小鼠体内显示出抗肿瘤活性[2]。 Animal Model: | ||||||||||||
| Name | Sepin-1 | ||||||||||||
| CAS | 163126-81-6 | ||||||||||||
| Formula | C9H9N3O4 | ||||||||||||
| Molar Mass | 223.19 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [1]. Zhang N, et al. Separase Inhibitor Sepin-1 Inhibits Foxm1 Expression and Breast Cancer Cell Growth. J Cancer Sci Ther. 2018;10(3):517. [2]. Zhang N, et al. Identification and Characterization of Separase Inhibitors (Sepins) for Cancer Therapy. J Biomol Screen. 2014 Jul;19(6):878-89. |