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Purity: ≥98%
Parthenolide, formerly known as NSC-157035, is a novel sesquiterpene lactone that was isolated from the herb feverfew with the potential to treat cancer. It works as an NF-κB activation inhibitor. In HeLa cells, parthenolide promotes apoptosis and growth inhibition via autophagy by inhibiting the PI3K/Akt signaling pathway, as well as mitochondrial membrane depolarization and ROS production.
| Targets |
HDAC1 ; NF-κB; MDM2; p53
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|---|---|
| ln Vitro |
Parthenolide (PTL), a sesquiterpene lactone isolated from feverfew shoots, inhibits the activity of the enzyme ubiquitin-specific peptidase 7 (USP7) and deubiquitinates and stabilizes β-catenin, the primary transcriptional factor of the Wnt signaling pathway, indicating that PTL is a promising anticancer agent that targets aberrant USP7/Wnt signaling.[4]
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| ln Vivo |
In a subcutaneous xenograft mouse model of gastric cancer (GC), parthenolide (PN), a P65 inhibitor, significantly increases tumor volumes that can be inhibited by gastrin.[5]
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| Cell Assay |
HEK293W cells are seeded in 96-well plates with three repeats and treated with PTL for 24 hours to confirm that PTL is a Wnt signaling inhibitor. HCT116 and SW480 cells are seeded in 96-well plates and transfected with Renilla reporter plasmid (8 ng/well) and SuperTOPFlash (80 ng/well), two luciferase reporter plasmids that are responsive to Wnt/-catenin signaling. Cells are transfected for 3 hours, given different PTL concentrations for 24 hours, and then lysed. Using the Dual-Luciferase Reporter Assay kit, the activities of both Firefly and Renilla luciferases are determined.
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| Animal Protocol |
Mice: They use Phb1 knockout mice. We treat males who are 8 to 12 weeks old. A dose of 3 mg/kg of parthenolide is intraperitoneally injected 24 hours and 1 hour prior to bile duct ligation (BDL) or twice weekly over a period of two weeks. For further analysis, liver specimens are quickly frozen.
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| References |
| Molecular Formula |
C15H20O3
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|---|---|
| Molecular Weight |
248.322
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| Exact Mass |
248.1412
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| Elemental Analysis |
C, 72.55; H, 8.12; O, 19.33
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| CAS # |
20554-84-1
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| Related CAS # |
20554-84-1
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| Appearance |
Solid powder
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| SMILES |
C/C/1=C\CC[C@@]2([C@H](O2)[C@@H]3[C@@H](CC1)C(=C)C(=O)O3)C
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| InChi Key |
KTEXNACQROZXEV-PVLRGYAZSA-N
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| InChi Code |
InChI=1S/C15H20O3/c1-9-5-4-8-15(3)13(18-15)12-11(7-6-9)10(2)14(16)17-12/h5,11-13H,2,4,6-8H2,1,3H3/b9-5+/t11-,12-,13+,15+/m0/s1
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| Chemical Name |
(1S,2R,4R,7E,11S)-4,8-dimethyl-12-methylidene-3,14-dioxatricyclo[9.3.0.02,4]tetradec-7-en-13-one
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| Synonyms |
Parthenolide; NSC 157035; NSC157035; NSC-157035
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~50 mg/mL (~201.4 mM)
Ethanol: ~50 mg/mL (~201.4 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.07 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: ≥ 2.08 mg/mL (8.38 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: 2% DMSO+corn oil: 10mg/mL |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00133341 | Completedg | Drug: Goldnatriomthiosulphate, MDBGN, parthenolide |
Allergic Contact Dermatitis | Mekos Laboratories AS | April 2005 | Phase 2 |
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