Cat. No.: HY-114936

Piericidin A

(Synonyms: AR-054)

5 Cited Publications

Customer Review

Based on 5 publication(s) in Google Scholar

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.

Purity: 99.83%
CAS No.: 2738-64-9
Formula: C₂₅H₃₇NO₄
Molecular Weight:415.57

Storage:

Solution, -20°C, 2 years

Piericidin A Chemical Structure

CAS No.: 2738-64-9

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Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (5)
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

All ADC Payloads Isoforms :

All Antibiotic Isoforms :

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]

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].

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

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].

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

Chemical Information

CAS No. 2738-64-9
Appearance Liquid
Molecular Weight 415.57
Formula C₂₅H₃₇NO₄
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
Synonyms

AR-054
Structure Classification
- Antibiotics
- Other Antibiotics
Initial Source
- Microorganisms
Streptomyces sp. BCC24731
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Solution, -20°C, 2 years

Publications (5)

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Sci Adv

Epstein-Barr virus-driven cardiolipin synthesis sustains metabolic remodeling during B cell transformation. [Abstract]

2025 Jan 31;11(5):eadr8837. PMID: 39879311
Sci Adv

Mitochondrial respiratory complex III sustains IL-10 production in activated macrophages and promotes tumor-mediated immune evasion. [Abstract]

2025 Jan 24;11(4):eadq7307. PMID: 39841829
PLoS Pathog

Epstein-Barr virus-transformed B-cells from a hypoxia model of the germinal center requires external unsaturated fatty acids. [Abstract]

2025 Nov 11;21(11):e1013694. PMID: 41218077
Res Sq

Epstein-Barr Virus-Driven B-Cell Transformation under Germinal Center Hypoxia Requires External Unsaturated Fatty Acids. [Abstract]

2025 Apr 24:rs.3.rs-6506954. PMID: 40313738
Res Sq

Epstein-Barr-Virus-Driven Cardiolipin Synthesis Sustains Metabolic Remodeling During B-cell Lymphomagenesis. [Abstract]

2024 Apr 8:rs.3.rs-4013392. PMID: 38659762

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (481 KB)
- English - EN (481 KB)
- Français - FR (481 KB)
- Deutsch - DE (481 KB)
- Norwegian - NO (481 KB)
- Español - ES (481 KB)
- Swedish - SV (481 KB)
- Italian - IT (481 KB)
- Korean - KR (481 KB)
- Portuguese - PT (481 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Matthias Höllerhage, et al. Piericidin A Aggravates Tau Pathology in P301S Transgenic Mice. PLoS One. 2014 Dec 1;9(12):e113557. [Content Brief]

[2]. Ji Eun Kang, et al. Efficacies of Quorum Sensing Inhibitors, Piericidin A and Glucopiericidin A, Produced by Streptomyces Xanthocidicus KPP01532 for the Control of Potato Soft Rot Caused by Erwinia Carotovora Subsp. Atroseptica. Microbiol Res. 2016 Mar;184:32-41. [Content Brief]

[3]. Solange Muhayimana, et al. Cytotoxic Selectivity and Apoptosis Induction of Piericidin A Contributes Potentially to Its Insecticidal Effect Against Mythimna Separata (Lepidoptera: Noctuidae) Larvae. Pestic Biochem Physiol. 2019 Jun;157:19-25. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Piericidin A

Publications Citing Use of MedChemExpress (MCE) Piericidin A

All ADC Payloads Isoforms

All Antibiotic Isoforms