LB100 是一种水溶性蛋白磷酸酶 2A (PP2A) 抑制剂。

LB-100 is a water soluble protein phosphatase 2A (PP2A) inhibitor. Phase 1.

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.

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%。

PP2A activity assays: Cultured pancreatic cancer cells are treated with IC50 of LB-100 for each cell line or equal volume of vehicle for 2 hours, and PP2A activity assays are then performed using Ser/Thr phosphatase assay kit. Cells are lysed with an ultrasonic cell disruptor, and the PP2A concentration is measured using a Ser/Thr phosphatase assay kit according to the instructions. Assays for each cell line are performed in triplicate.

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)

1632032-53-1

C13H20N2O4

268.313

LB 100;LB-100

DMSO:<1 mgml
Ethanol:<1 mgml
H2O:49 mg/mL (182.6 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years