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CAS No. : 2738-64-9
MCE 国际站:Piericidin A
产品活性:Piericidin A (AR-054) 是一种天然线粒体 NADH-泛醌氧化还原酶 (复合物 I; complex I) 抑制剂。Piericidin A 是一种有效的神经毒素,通过其对 NADH-泛醌还原酶 (NADH-ubiquinone reductase) 的作用破坏电子传输系统,从而抑制线粒体呼吸。Piericidin A 还是一种潜在的群体感应抑制剂,可抑制胡萝卜欧文氏菌亚种 atroseptica (Eca) 的毒力基因的表达。Piericidin A 是一种 ADC 细胞毒素,具有抗菌,抗癌,杀虫活性。
研究领域:Anti-infection | Antibody-drug Conjugate/ADC Related | Metabolic Enzyme/Protease
作用靶点:Bacterial | ADC Cytotoxin | Antibiotic | Mitochondrial Metabolism
结构分类:抗生素 | 疾病研究 | 抗菌 | 抗生素 | 疾病研究 | 抗癌 | 抗生素 | 疾病研究 | 抗虫 | 抗生素 | 其他类 | 结构分类
In Vitro: In a cell free assay, the potency of Piericidin A to inhibit mitochondrial complex I is ∼2 fold smaller than the one of annonacin. In cultured neurons, Piericidin A potently induces the redistribution of phosphorylated tau from the dendrites into the cell soma and induces cell death.
The viability of Tn5B1-4 cells is inhibited by Piericidin A in a time- and concentration-dependent manner with IC50 value of 0.061 μM, whilst Piericidin A shows slight inhibitory effect on the viability of HepG2 and Hek293 cells with IC50 value of 233.97 μM and 228.96 μM, respectively. Piericidin A induces apoptosis of Tn5B1-4 cells coincides with a decrease in the mitochondrial membrane potential.
In Vivo: Piericidin A (0.5 mg/kg/d; for 28 days via osmotic minipumps) significantly increases the number of phospho-tau immunoreactive cells in the cerebral cortex in P301S+/+ mice. Piericidin A leads to increased levels of pathologically phosphorylated tau only in P301S+/+ mice. The synaptic density is reduced by Piericidin A treatment in P301S+/+ mice. Exposure to Piericidin A aggravates the course of genetically determined tau pathology.
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货号: HY-114936
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