2. Anti-infection Antibody-drug Conjugate/ADC Related Metabolic Enzyme/Protease
  3. Bacterial ADC Payload 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 技术支持

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

Piericidin A Chemical Structure

CAS No. : 2738-64-9

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1 mg (12.03 mM * 200 μL in Ethanol) ￥4500
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Piericidin A 相关抗体

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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)

在无细胞实验中，Piericidin A 抑制线粒体复合物 I 的效力比 annonacin 低约 2 倍。在培养的神经元中，Piericidin A 强效诱导磷酸化 tau 从树突重新分布到细胞体，并诱导细胞死亡[1]。
Piericidin A 以时间和浓度依赖性方式抑制 Tn5B1-4 细胞的活力，IC50 值为 0.061 μM，而 Piericidin A 对 HepG2 和 Hek293 细胞的活力有轻微抑制作用，IC50 值分别为 233.97 μM 和 228.96 μM。 Piericidin A 诱导 Tn5B1-4 细胞凋亡，与线粒体膜电位降低同时发生[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；通过渗透性微泵给药，持续 28 天) 显著增加了 P301S+/+ 小鼠大脑皮层中磷酸化 tau 免疫反应细胞的数量。Piericidin A 仅导致 P301S+/+ 小鼠中病理性磷酸化 tau 水平升高。Piericidin A 治疗 P301S+/+ 小鼠的突触密度降低。暴露于 Piericidin A 会加剧基因决定的 tau 病理进程[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 PayloadAntibioticMitochondrial MetabolismADC CytotoxinInhibitorinhibitorinhibit

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