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Parthenolide

Catalog No. T2140   CAS 20554-84-1
Synonyms: (-)-Parthenolide

(-)-Parthenolide ((-)-Parthenolide), an inhibitor of the Nuclear Factor-κB Pathway, also promotes the ubiquitination of MDM2 and activates p53 cellular functions.

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Parthenolide Chemical Structure
Parthenolide, CAS 20554-84-1
Pack Size Availability Price/USD Quantity
50 mg In stock $ 50.00
100 mg In stock $ 68.00
200 mg In stock $ 119.00
1 mL * 10 mM (in DMSO) In stock $ 50.00
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Purity: 99.46%
Purity: 99.33%
Purity: 99.10%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description (-)-Parthenolide ((-)-Parthenolide), an inhibitor of the Nuclear Factor-κB Pathway, also promotes the ubiquitination of MDM2 and activates p53 cellular functions.
In vitro Parthenolide (PTL) has a dose-dependent growth inhibition effect on NSCLC cells Calu-1, H1792, A549, H1299, H157, and H460. Parthenolide can induce cleavage of apoptotic proteins such as CASP8, CASP9, CASP3 and PARP1 both in concentration- and time-dependent manner in tested lung cancer cells which indicates that apoptosis is trigged after Parthenolide exposure. Besides induction of apoptosis, Parthenolide also induces G0/G1 cell cycle arrest in a concentration-dependent manner in A549 cells and G2/M cell cycle arrest in H1792 cells[2].
In vivo Parthenolide, an HDAC inhibitor with anti-inflammatory properties, demonstrated significant anti-apoptotic effects in Phb1 KO hepatocytes. This compound, when administered alongside TSA, increased FXR levels while decreasing CYP7A1, HDAC4, TNFα, TRAIL, and Bax levels. This suggests that Parthenolide's specific HDAC inhibition might reduce bile acid toxicity, thereby attenuating the apoptotic response in Phb1 KO hepatocytes. Remarkably, Parthenolide also offered protection against liver injury in Phb1 KO mice post-bile duct ligation (BDL), as evidenced by a reduction in mortality rates, lower apoptotic responses, decreased necrotic areas, reduced Tunel-staining, and significantly lower ALT (8431±957 vs. 4225±210 U/L) and AST (4805±300 vs. 2242±438 U/L) levels compared to control Phb1 KO mice.
Cell Research Parthenolide (PTL) is dissolved in DMSO and diluted with appropriate media[2]. Cells are seeded in 96-well plates and treated on the second day with the given concentration of Parthenolide (0, 5, 10, 20 μM) for another 48 hours and then subjected to SRB or MTT assay. For SRB assay, live cell number is estimated as described earlier. After treatment, the medium is discarded firstly. In order to fix the adherent cells, 100 μL of cold trichloroacetic acid (10% (w/v)) are adding to each well and incubating at 4°C for at least 1 hour. The plates are then washed five times with deionized water and dried in the air. Each well are then added with 50 μL of SRB solution (0.4% w/v in 1% acetic acid) and incubated for 5 min at room temperature. The plates are washed five times with 1% acetic acid to remove unbound SRB and then air dried. The residual bound SRB is solubilized with 100 μL of 10 mM Tris base buffer (pH 10.5), and then read using a microtiter plate reader at 495 nm. The MTT assay is executed. 20 μL MTT (5 mg/mL) are added to each sample and incubate at 37°C for 4 h, then 100 μL solubilization solution are added. Cell viability is determined at 595 nm[2].
Source
Synonyms (-)-Parthenolide
Molecular Weight 248.32
Formula C15H20O3
CAS No. 20554-84-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 49 mg/mL (197.33 mM)

Ethanol: 50 mg/mL (201.35 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Nakshatri, H., Appaiah, H., Anjanappa, M., Gilley, D., Tanaka, H., & Badve, S. et al. (2015). NF-κB-dependent and -independent epigenetic modulation using the novel anti-cancer agent DMAPT. Cell Death & Disease, 6(1), e1608-e1608. doi: 10.1038/cddis.2014.569 2. Zhao X, et al. Parthenolide induces apoptosis via TNFRSF10B and PMAIP1 pathways in human lung cancer cells. J Exp Clin Cancer Res. 2014 Jan 6;33:3. 3. Barbier-Torres L, et al. Histone deacetylase 4 promotes cholestatic liver injury in the absence of prohibitin-1. Hepatology. 2015 Oct;62(4):1237-48.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Drug Repurposing Compound Library Traditional Chinese Medicine Monomer Library Anti-Colorectal Cancer Traditional Chinese Medicine Compound Library Anti-Pancreatic Cancer Compound Library Antidepressant Compound Library Anti-Breast Cancer Compound Library Natural Product Library

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Keywords

Parthenolide 20554-84-1 Apoptosis Autophagy Chromatin/Epigenetic DNA Damage/DNA Repair NF-Κb Mitophagy NF-κB HDAC inhibit (-)-Parthenolide Nuclear factor-kappaB Mitochondrial Autophagy Nuclear factor-κB Inhibitor inhibitor

 

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