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)

製品番号: HY-114936 純度: 99.83%
COA 取扱説明書 Technical Support

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.

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Piericidin A

Piericidin A 構造式

CAS 番号 : 2738-64-9

容量 価格（税別） 在庫状況 数量
Solvent
1 mg (12.03 mM * 200 μL in Ethanol) USD 650 在庫あり
Solvent
5 mg (12.03 mM * 1 mL in Ethanol) USD 1774 在庫あり

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カスタマーレビュー

Based on 5 publication(s) in Google Scholar

Piericidin A 関連抗体

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製品説明

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].

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]
BTI-TN-5B1-4 IC50
61 nM
Compound: 9
Cytotoxicity against Trichoplusia ni BTI-TN-5B1-4 cells assessed as reduction cell proliferation incubated for 24 hrs by MTT assay
Cytotoxicity against Trichoplusia ni BTI-TN-5B1-4 cells assessed as reduction cell proliferation incubated for 24 hrs by MTT assay
[PMID: 36893622]
HEK293 IC50
228.96 μM
Compound: 9
Cytotoxicity against human HEK293 cells assessed as reduction in cell proliferation incubated for 24 hrs by MTT assay
Cytotoxicity against human HEK293 cells assessed as reduction in cell proliferation incubated for 24 hrs by MTT assay
[PMID: 36893622]
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]
HepG2 IC50
233.97 μM
Compound: 9
Cytotoxicity against human HepG2 cells assessed as reduction cell proliferation incubated for 24 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction cell proliferation incubated for 24 hrs by MTT assay
[PMID: 36893622]
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]
HT-29 IC50
6.4 nM
Compound: 9
Inhibition of colony formation of human HT-29 cells assessed as reduction in colonies incubated for 7 days by crystal violet staining based analysis
Inhibition of colony formation of human HT-29 cells assessed as reduction in colonies incubated for 7 days by crystal violet staining based analysis
[PMID: 36893622]
HT-29 IC50
7.7 nM
Compound: 9
Inhibition of colony formation of human HT-29 cells incubated for 7 days in absence of glucose by crystal violet staining based analysis
Inhibition of colony formation of human HT-29 cells incubated for 7 days in absence of glucose by crystal violet staining based analysis
[PMID: 36893622]
L929 IC50
0.43 nM
Compound: 5, piericidin A1
Cytotoxicity against mouse L929 fibroblasts
Cytotoxicity against mouse L929 fibroblasts
[PMID: 18054490]
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]
体外実験

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].

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

Piericidin A 関連抗体
体内実験

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].

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

415.57

分子式

C25H37NO4
CAS 番号
Appearance

Liquid

Color

Colorless to light yellow

SMILES

COC1=C(C(C)=C(N=C1OC)C/C=C(C/C=C/C(C)=C/[C@@H](C)[C@H](/C(C)=C/C)O)\C)O
Structure Classification
Initial Source

Streptomyces sp. BCC24731
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Solution, -20°C, 2 years
純度とドキュメンテーション

純度: 99.83%

COA (244 KB) RP-HPLC (257 KB)

取扱説明書 (2659 KB)
参考文献
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Piericidin A Related Classifications

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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-054AR054AR 054BacterialADC PayloadAntibioticMitochondrial MetabolismADC CytotoxinInhibitorinhibitorinhibit

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Piericidin A
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HY-114936
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