化合物LB100 T4449

Product Introduction
Bioactivity


英文名: LB100

描述: LB100 (LB-100) 是一种水溶性蛋白磷酸酶 2A(PP2A) 抑制剂。

细胞实验: 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)

激酶实验: 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.

体外活性: 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.

体内活性: 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%。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : 49 mg/mL (182.6 mM)
DMSO : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)


关键字: LB100

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相关库: Glycometabolism Compound Library | Anti-Obesity Compound Library | Lipid Metabolism Compound Library | NO PAINS Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途