Home NF-κB HDAC inhibitor - NF-κB inhibitor - MDM2/MDMX activator - p53 activator (-)-Parthenolide For research use only.

(-)-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

HDAC Signaling Pathways

HDAC 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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