(-)-Parthenolide

Catalog No.S2341 Batch:S234107

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Technical Data

Formula

C15H20O3
Molecular Weight 248.32 CAS No. 20554-84-1
Solubility (25°C)* In vitro DMSO 49 mg/mL (197.32 mM)
Ethanol 49 mg/mL (197.32 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 (-)-Parthenolide, an inhibitor of the Nuclear Factor-κB Pathway, specifically depletes HDAC1 protein without affecting other class I/II HDACs; Also promotes the ubiquitination of MDM2 and activates p53 cellular functions.
Targets
HDAC1 [1] NF-κB [2] MDM2 [3] p53 [3]
In vitro

Parthenolide (PTL), a sesquiterpene lactone purified from the shoots of the feverfew, inhibits ubiquitin-specific peptidase 7 (USP7) activity and deubiquitinate and stabilize β-catenin which the key transcriptional factor of Wnt signaling pathway, suggesting that PTL is an promising anticancer agent targeting aberrant USP7/Wnt signaling.[4]
In vivo

Parthenolide (PN), a P65 inhibitor, significantly increases the tumor volumes in subcutaneous xenograft gastric cancer (GC) mouse model, which can be reversed by gastrin.[5]

Protocol (from reference)

Cell Assay:

[4]
  • Cell lines

    HCT116, SW480, HEK293W cells

  • Concentrations

    2.5, 5.0, 10 μM

  • Incubation Time

    24 h

  • Method

    To confirm PTL as a Wnt signaling inhibitor, HEK293W cells are seeded in 96-well plates with three repeats and treated with PTL for 24 h. HCT116 and SW480 cells are seeded in 96-well plates and then transfected as follows: Wnt/β-catenin signaling responsive Firefly luciferase reporter plasmid SuperTOPFlash (80 ng/well) and Renilla reporter plasmid (8 ng/well). After 3-h transfection, cells are exposed to various concentrations of PTL for 24 h and then lysed. Both Firefly and Renilla luciferase activities are measured using the Dual-Luciferase Reporter Assay kit.
Animal Study:

[5]
  • Animal Models

    Female athymic BALB/c nude mice of xenograft gastric cancer (GC) model

  • Dosages

    4 mg/kg/day

  • Administration

    --

Customer Product Validation

, , Harvard University, 2014.

Data from [Data independently produced by , , Cell Oncol (Dordr), 2017, 40(3):263-279]

Data from [Data independently produced by , , J Neuroimmunol, 2017, 305:154-161]

Selleck's (-)-Parthenolide has been cited by 22 publications

Connexin43 is associated with the progression of clear cell renal carcinoma and is regulated by tangeretin to sygergize with tyrosine kinase inhibitors [ Transl Oncol, 2023, 35:101712] PubMed: 37354638
Histone deacetylase 1 controls cardiomyocyte proliferation during embryonic heart development and cardiac regeneration in zebrafish [ PLoS Genet, 2021, 17(11):e1009890] PubMed: 34723970
Reduced Mitochondrial Apoptotic Priming Drives Resistance to BH3 Mimetics in Acute Myeloid Leukemia [ Cancer Cell, 2020, 38(6):872-890.e6] PubMed: 33217342
Lack of FGF21 promotes NASH-HCC transition via hepatocyte-TLR4-IL-17A signaling [ Theranostics, 2020, 10(22):9923-9936] PubMed: 32929325
Parthenolide inhibits ubiquitin-specific peptidase 7 (USP7), Wnt signaling, and colorectal cancer cell growth. [ J Biol Chem, 2020, 295(11):3576-3589] PubMed: 32029476
Parthenolide Inhibits Angiogenesis in Esophageal Squamous Cell Carcinoma Through Suppression of VEGF [ Onco Targets Ther, 2020, 13:7447-7458] PubMed: 32801767
Loss of N-Glycanase 1 Alters Transcriptional and Translational Regulation in K562 Cell Lines [ G3 (Bethesda), 2020, 4;10(5):1585-1597] PubMed: 32265286
An antiviral drug screening system for enterovirus 71 based on an improved plaque assay: A potential high-throughput method [ J Med Virol, 2019, 91(8):1440-1447] PubMed: 30900754
SIRT3 deacetylase activity confers chemoresistance in AML via regulation of mitochondrial oxidative phosphorylation. [ Br J Haematol, 2019, 187(1):49-64] PubMed: 31236919
Novel Targeted Nano-Parthenolide Molecule against NF-kB in Acute Myeloid Leukemia. [ Molecules, 2019, 24(11)] PubMed: 31163672

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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.

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