| Description | LB100 (LB-100) is a water soluble protein phosphatase 2A (PP2A) inhibitor. |
| In vitro | 在胰腺癌异种移植小鼠模型中, LB-100（2 mg/kg,i.p.）可增加化疗药物阿霉素的疗效.LB-100使肿瘤表面血流速度和肿瘤微血管密度增加. |
| In vivo | 与对照组相比,LB-100使细胞内阿霉素浓度升高约2.5倍,并增加肿瘤细胞对阿霉素的敏感性。LB-100使血管内皮生长因子分泌增加,从而促进HIF-1α-VEGF介导的血管生成。LB-100对BxPc-3（IC50：2.3 μM）和Panc-1（IC50：1.7 μM）细胞的生长有明显抑制效果。经LB-100处理后,BxPc-3、SW1990和Panc-1细胞肿的PP2A活性下降30-50%。 |
| Cell experiments | Cytotoxicity is conducted by using a Cell Counting Kit-8. Cells are seeded in 96-well plates with a density of 3000 cells per well and are assessed after treatments following the CCK-8 protocol. Relative cytotoxicity is expressed as a percentage of speci?c controls. (Only for Reference) |
| Target activity | PP2A(BxPc-3):0.85 μM, PP2A(Panc-1):3.87 μM |
| Synonyms | LB-100, LB 100 |
| molecular weight | 268.31 |
| Molecular formula | C13H20N2O4 |
| CAS | 1632032-53-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: 49 mg/mL (182.6 mM) DMSO: < 1 mg/mL (insoluble or slightly soluble) Ethanol: < 1 mg/mL (insoluble or slightly soluble) |
| References | 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 |
| Citations | 1. Zhang J, Cen L, Zhang X, et al. MPST deficiency promotes intestinal epithelial cell apoptosis and aggravates inflammatory bowel disease via AKT. Redox Biology. 2022: 102469. |