(-)-Parthenolide

Catalog No.S2341

For research use only.

(-)-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.

(-)-Parthenolide Chemical Structure

CAS No. 20554-84-1

Selleck's (-)-Parthenolide has been cited by 20 publications

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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]

Assay
Methods Test Index PMID
Growth inhibition assay Cell viability 28423582
Western blot B-Raf / c-Myc ; MEK / p-MEK / ERK / p-ERK ; STAT3 / p-STAT3 / GSK3α/β / AKT / p-AKT ; Bcl-2 / Bak / Bax 28423582 23039130
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 Research:

[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 Research:

[5]

  • Animal Models: Female athymic BALB/c nude mice of xenograft gastric cancer (GC) model
  • Dosages: 4 mg/kg/day
  • Administration: --

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+corn oil
For best results, use promptly after mixing.

10mg/mL

Chemical Information

Molecular Weight 248.32
Formula

C15H20O3

CAS No. 20554-84-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CCCC2(C(O2)C3C(CC1)C(=C)C(=O)O3)C

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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