2. Anti-infection Antibody-drug Conjugate/ADC Related Metabolic Enzyme/Protease
  3. Bacterial ADC Cytotoxin Antibiotic Mitochondrial Metabolism
  4. Piericidin A

Piericidin A  (Synonyms: AR-054)

目录号: HY-114936 纯度: ≥99.0%
COA 产品使用指南

摩尔计算器

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。

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Piericidin A Chemical Structure

Piericidin A Chemical Structure

CAS No. : 2738-64-9

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规格 价格 是否有货 数量
1 mg (12.03 mM * 200 μL in Ethanol) ￥4500
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Piericidin A 相关抗体

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MCE 顾客使用本产品发表的 1 篇科研文献

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Piericidin A (AR-054) is a natural mitochondrial NADH-ubiquinone oxidoreductase (complex I) inhibitor. Piericidin A is a potent neurotoxin and inhibits mitochondrial respiration by disrupting the electron transport system through its action on NADH-ubiquinone reductase. Piericidin A is also a potential quorum-sensing inhibitor that suppresses the expression of the virulence genes of Erwinia carotovora subsp. atroseptica (Eca). Piericidin A is an ADC cytotoxin and has anti-bacterial, anticancer, insecticidal activity[1][2][2].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
786-0 IC50
30 μM
Compound: 1; PA
Cytotoxicity against human 786-O cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
Cytotoxicity against human 786-O cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
[PMID: 31298537]
ACHN IC50
0.4 μM
Compound: 1; PA
Cytotoxicity against human ACHN cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
Cytotoxicity against human ACHN cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
[PMID: 31298537]
ACHN IC50
1.6 μM
Compound: 1; PA
Cytotoxicity against human ACHN cells harboring shPRDX1 gene assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
Cytotoxicity against human ACHN cells harboring shPRDX1 gene assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
[PMID: 31298537]
HeLa IC50
84.9 μM
Compound: 6
Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay
Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay
[PMID: 28406643]
HK-2 IC50
> 100 μM
Compound: 1; PA
Cytotoxicity against human HK2 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
Cytotoxicity against human HK2 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
[PMID: 31298537]
HL-60 IC50
82.1 μM
Compound: 6
Antiproliferative activity against human HL60 cells after 48 hrs by EZ-Cytox cell viability assay
Antiproliferative activity against human HL60 cells after 48 hrs by EZ-Cytox cell viability assay
[PMID: 28406643]
MDA-MB-231 IC50
> 100 μM
Compound: 6
Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay
[PMID: 28406643]
OS-RC-2 IC50
5.2 μM
Compound: 1; PA
Cytotoxicity against human OS-RC2 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
Cytotoxicity against human OS-RC2 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
[PMID: 31298537]
SW480 IC50
82.1 μM
Compound: 6
Antiproliferative activity against human SW480 cells after 48 hrs by MTT assay
Antiproliferative activity against human SW480 cells after 48 hrs by MTT assay
[PMID: 28406643]
U2OS IC50
91.5 μM
Compound: 6
Antiproliferative activity against human U2OS cells after 48 hrs by MTT assay
Antiproliferative activity against human U2OS cells after 48 hrs by MTT assay
[PMID: 28406643]
体外研究
(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[1].
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[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Piericidin A 相关抗体:
体内研究
(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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

415.57

Formula

C25H37NO4
CAS 号
性状

液体

颜色

Colorless to light yellow

中文名称

粉蝶霉素A
结构分类
初始来源

Streptomyces sp. BCC24731
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Solution, -20°C, 2 years
纯度 & 产品资料

纯度: ≥99.0%

COA (280 KB)

产品使用指南 (1538 KB)
参考文献

Piericidin A 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Piericidin A2738-64-9AR-054粉蝶霉素AAR054AR 054BacterialADC CytotoxinAntibioticMitochondrial MetabolismADC PayloadInhibitorinhibitorinhibit

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