1. Anti-infection
    Antibody-drug Conjugate/ADC Related
  2. Bacterial
    ADC Cytotoxin
    Antibiotic
  3. Piericidin A

Piericidin A (Synonyms: AR-054)

Cat. No.: HY-114936
Handling Instructions

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.

For research use only. We do not sell to patients.

Piericidin A Chemical Structure

Piericidin A Chemical Structure

CAS No. : 2738-64-9

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Description

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].

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].

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].

Molecular Weight

415.57

Formula

C₂₅H₃₇NO₄

CAS No.

2738-64-9

SMILES

COC1=C(C(C)=C(N=C1OC)C/C=C(C/C=C/C(C)=C/[[email protected]@H](C)[[email protected]](/C(C)=C/C)O)\C)O

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

Piericidin AAR-054AR054AR 054BacterialADC CytotoxinAntibioticTaumitochondrialcomplex Ilipophilictauopathiesanticanceranti-bacterialneurotoxinADCcytotoxinInhibitorinhibitorinhibit

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