(-)-Parthenolide

(-)-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

(-)-Parthenolide Chemical Structure

CAS No. 20554-84-1

Purity & Quality Control

(-)-Parthenolide Related Products

Signaling Pathway

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
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]

Cell Research 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.

Experimental Result Images Methods Biomarkers Images 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
In Vivo
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]

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

Chemical Information & Solubility

Molecular Weight 248.32 Formula

C15H20O3

CAS No. 20554-84-1 SDF Download (-)-Parthenolide SDF
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 50 mg/mL ( (201.35 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 50 mg/mL

Water : Insoluble


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In vivo
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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.

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