1. NF-κB
    Cell Cycle/DNA Damage
    Epigenetics
    Autophagy
  2. NF-κB
    HDAC
    DNA Methyltransferase
    Autophagy

Parthenolide (Synonyms: (-)-Parthenolide)

Cat. No.: HY-N0141 Purity: 99.13%
Data Sheet SDS Handling Instructions

Parthenolide is an NF-κB inhibitor, reduces histone deacetylase 1 (HDAC-1) and DNA methyltransferase 1 independent of NF-κB inhibition.

For research use only. We do not sell to patients.
Parthenolide Chemical Structure

Parthenolide Chemical Structure

CAS No. : 20554-84-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $55 In-stock
50 mg $50 In-stock
100 mg $70 In-stock
200 mg $120 In-stock
500 mg   Get quote  
1 g   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Parthenolide is an NF-κB inhibitor, reduces histone deacetylase 1 (HDAC-1) and DNA methyltransferase 1 independent of NF-κB inhibition.

IC50 & Target

NF-κB, HDAC1, DNA Methyltransferase[1]

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, indicating that apoptosis is trigged after Parthenolide exposure. In addition to 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

Only Parthenolide, the HDAC inhibitor with anti-inflammatory features, displayed a potent anti-apoptotic effect in Phb1 KO hepatocytes. Indeed, TSA and Parthenolide-treated hepatocytes showed increased levels of FXR, and reduced levels of CYP7A1, HDAC4, TNFα, TRAIL and Bax suggesting a less toxic effect of bile acids as a results of specific HDAC inhibition, resulting in the attenuation of the Phb1 KO hepatocytes apoptotic response. Importantly, Parthenolide exerts a protective effect from the liver injury after BDL in Phb1 KO mice. Indeed, Parthenolide treatment results in a reduction of the mortality rate of this mice after BDL associated with a lower apoptotic response as revealed by a reduction of necrotic areas, Tunel-staining, as well as decreased ALT (8431±957 vs.4225±210 U/L) and AST (4805±300 vs.2242±438 U/L) activities compared to control Phb1 KO mice[3].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00133341 Mekos Laboratories AS Allergic Contact Dermatitis April 2005 Phase 2
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 4.0271 mL 20.1353 mL 40.2706 mL
5 mM 0.8054 mL 4.0271 mL 8.0541 mL
10 mM 0.4027 mL 2.0135 mL 4.0271 mL
Cell Assay
[2]

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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

Mice[3]
Phb1 KO animals are used. Males from 8-12 weeks of age are treated. Parthenolide is intraperitoneally injected at a dose of 3mg/kg 24 h and 1h before bile duct ligation (BDL) or twice a week during two weeks. Liver specimens are snap-frozen for subsequent analysis. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

248.32

Formula

C₁₅H₂₀O₃

CAS No.

20554-84-1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Parthenolide
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