| Bioactivity | LB-100 is a protein phosphatase 2A (PP2A) inhibitor, with IC50 of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells[1][2][3]. | ||||||||||||
| Target | IC50: 0.85 μM (PP2 in BxPc-3 cell), 3.87 μM (PP2 in Panc-1 cell) | ||||||||||||
| Invitro | LB-100 抑制细胞生长，IC50 分别为 2.3 μM (BxPc-3)和 1.7 μM (Panc-1)。在 BxPc-3、Panc-1 和 SW1990 细胞中，LB-100 可使 PP2A 活性降低 30-50%。LB-100 增加细胞内阿霉素的浓度(对照 2.5 倍)，并使肿瘤细胞对阿霉素的细胞毒性敏感。LB-100 增加 VEGF 分泌，从而增强 HIF-1α-VEGF 介导的血管生成[1]。LB-100 改变内皮细胞间 ve-钙粘蛋白的完整性。LB-100 的预处理结果使通过 HUVECs 单层的染料增加了近 40%。LB-100 诱导血管内皮细胞细胞旁通透性升高，这可能是 LB-100 增加肿瘤细胞中阿霉素浓度的原因[2]。LB-100 下调 Bcl-2 表达，增强索拉非尼诱导的 HCC 细胞凋亡[3]。 | ||||||||||||
| In Vivo | LB-100 (2 mg/kg,腹腔注射) 以时间依赖性的方式降低裸鼠异种移植物和肝脏中 PP2A 的活性。经免疫印迹证实，LB-100 不会改变三种 PP2A 亚基 (PP2A_A、PP2A_B 和 PP2A_C) 在细胞系、异种移植物或肝脏中的表达。阿霉素(1.5 kg/mL，每隔一天) 和 LB-100 (2 mg/kg，每隔一天) 联合用药可显著减缓两种动物的肿瘤生长，缩小肿瘤体积，而单药处理对动物的肿瘤生长无影响[2]。 | ||||||||||||
| Name | LB-100 | ||||||||||||
| CAS | 1632032-53-1 | ||||||||||||
| Formula | C13H20N2O4 | ||||||||||||
| Molar Mass | 268.31 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Bai X, et al. Inhibition of protein phosphatase 2A sensitizes pancreatic cancer to chemotherapy by increasing drug perfusion via HIF-1α-VEGF mediated angiogenesis. Cancer Lett. 2014 Oct 7. pii: S0304-3835(14)00589-8. [2]. Bai XL, et al. Inhibition of protein phosphatase 2A enhances cytotoxicity and accessibility of chemotherapeutic drugs to hepatocellular carcinomas. Mol Cancer Ther. 2014 Aug;13(8):2062-72. [3]. Fu QH, et al. LB-100 sensitizes hepatocellular carcinoma cells to the effects of sorafenib during hypoxia by activation of Smad3 phosphorylation. Tumour Biol. 2016 Jun;37(6):7277-8 |