Piperlongumine

Catalog No.S7551 Batch:S755103

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Technical Data

Formula

C17H19NO5
Molecular Weight 317.34 CAS No. 20069-09-4
Solubility (25°C)* In vitro DMSO 63 mg/mL (198.52 mM)
Ethanol 5 mg/mL (15.75 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Piperlongumine (PPLGM, Piplartine), a natural alkaloid from Piper longum L., increases the level of reactive oxygen species (ROS) and selectively kills cancer cells. It is a direct TrxR1 inhibitor with suppressive activity against gastric cancer and a novel inhibitor of CRM1; also an inhibitor of PI3K/Akt/mTOR in human breast cancer cells.
Targets
reactive oxygen species (ROS) [1] TrxR1 [5] CRM1 [6] PI3K/Akt/mTOR [7]
In vitro Piperlongumine is a known ROS inducer which could induce pancreatic cancer cell death in cell culture[1] As a thromboxane A(2) receptor antagonist, Piperlongumine inhibits platelet aggregation. [2] Piperlongumine also promotes autophagy via inhibition of Akt/mTOR signalling and mediates cancer cell death. [3]
In vivo Piperlongumine (50 mg/kg i.p.) causes in vivo growth inhibition of tumor cells without leading to major changes in the biochemical, hematological and histopathological parameters. [4]

Protocol (from reference)

Cell Assay:

[3]
  • Cell lines

    MCF-7 and 786-O cells

  • Concentrations

    ~10 μM

  • Incubation Time

    48 hours

  • Method

    MCF-7 and 786-O cells are incubated with various PL concentrations for 48h. Cell proliferation is analysed by CellTiter Blue assay. Effective doses (ED) are calculated using XLift, Microsoft Excel add-in.
Animal Study:

[4]
  • Animal Models

    Mice transplanted with sarcoma 180 tumors

  • Dosages

    ~50 mg/kg

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by , , Oncotarget, 2016, 7(35):56933-56943]

Data from [Data independently produced by , , Oncotarget, 2016, 7(26):40531-40545]

Selleck's Piperlongumine has been cited by 26 publications

Anti-cancer agent piperlongumine is an inhibitor of transient receptor potential melastatin 7 channel in oral squamous cell carcinoma [ J Oral Biosci, 2024, S1349-0079(24)00071-9] PubMed: 38452870
Piperlongumine conquers temozolomide chemoradiotherapy resistance to achieve immune cure in refractory glioblastoma via boosting oxidative stress-inflamation-CD8+-T cell immunity [ J Exp Clin Cancer Res, 2023, 42(1):118] PubMed: 37161450
Identification of Piperlongumine as Potent Inhibitor of Necroptosis [ Drug Des Devel Ther, 2023, 17:1387-1394] PubMed: 37188283
Grainyhead 1 acts as a drug-inducible conserved transcriptional regulator linked to insulin signaling and lifespan [ Nat Commun, 2022, 13(1):107] PubMed: 35013237
USP5-Beclin 1 axis overrides p53-dependent senescence and drives Kras-induced tumorigenicity [ Nat Commun, 2022, 13(1):7799] PubMed: 36528652
Systematic identification of biomarker-driven drug combinations to overcome resistance [ Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7] PubMed: 35332332
Screening Health-Promoting Compounds for Their Capacity to Induce the Activity of FOXO3 [ J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493] PubMed: 34508571
A "Failed" Assay Development for the Discovery of Rescuing Small Molecules from the Radiation Damage [ SLAS Discov, 2021, 24725552211020678] PubMed: 34151632
MLH1 Deficiency Induces Cetuximab Resistance in Colon Cancer via Her-2/PI3K/AKT Signaling [ Adv Sci (Weinh), 2020, 7(13):2000112] PubMed: 32670759
Engineering Chromosome Region Maintenance 1 Fragments That Bind to Nuclear Export Signals [ Protein Sci, 2020, 29(6):1366-1372] PubMed: 31495993

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.