(-)-Parthenolide

製品コードS2341 バッチS234109

印刷

化学情報

 Chemical Structure Synonyms N/A Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C15H20O3

分子量 248.32 CAS No. 20554-84-1
Solubility (25°C)* 体外 DMSO 50 mg/mL (201.35 mM)
Ethanol (warmed with 50ºC water bath) 50 mg/mL (201.35 mM)
Water Insoluble
体内 (毎回新しく調製した物を用意してください)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

2.500mg/ml (10.07mM) Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 Nuclear Factor-κB経路の阻害剤である(-)-Parthenolideは、他のクラスI/II HDACsに影響を与えることなく、HDAC1タンパク質を特異的に枯渇させます。また、MDM2のユビキチン化を促進し、p53細胞機能を活性化します。
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.

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.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HCT116, SW480, HEK293W cells
濃度 2.5, 5.0, 10 μM
反応時間 24 h
実験の流れ

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.

動物実験 動物モデル Female athymic BALB/c nude mice of xenograft gastric cancer (GC) model
投薬量 4 mg/kg/day
投与方法 --

参考

  • https://pubmed.ncbi.nlm.nih.gov/17656318/
  • https://pubmed.ncbi.nlm.nih.gov/11961112/
  • https://pubmed.ncbi.nlm.nih.gov/19276167/
  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7076227/
  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5987590/

カスタマーフィードバック

, , Harvard University, 2014.

Data from [Data independently produced by , , Cell Oncol (Dordr), 2017, 40(3):263-279]

Data from [Data independently produced by , , J Neuroimmunol, 2017, 305:154-161]

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

Ketogenic diet and β-hydroxybutyrate inhibit HDAC1 to preserve vascular smooth muscle cell function in thoracic aortic aneurysm [ J Adv Res, 2025, S2090-1232(25)00353-4] PubMed: 40398746
Synergistic activity of S63845 and parthenolide to overcome acquired resistance to MEK1/2 inhibitor in melanoma cells: Mechanisms and therapeutic potential [ Biomed Pharmacother, 2025, 188:118183] PubMed: 40424823
Development of translational read-through-inducing drugs as novel therapeutic options for patients with Fanconi anemia [ Cell Death Discov, 2025, 11(1):286] PubMed: 40544182
TNFSF14-HVEM/LTβR Exacerbates Keratinocyte Abnormalities and IMQ-Induced Psoriatic Skin Inflammation via Activating NF-κB/TWIST1 Signalling Pathway [ J Cell Mol Med, 2025, 29(15):e70774] PubMed: 40768619
Astaxanthin suppresses the malignant behaviors of nasopharyngeal carcinoma cells by blocking PI3K/AKT and NF-κB pathways via miR-29a-3p [ Genes Environ, 2024, 46(1):10] PubMed: 38649975
Parthenolide Targets NLRP3 to Treat Inflammasome-Related Diseases [ Int Immunopharmacol, 2023, 119:110229.] PubMed: 37167640
Connexin43 is associated with the progression of clear cell renal carcinoma and is regulated by tangeretin to sygergize with tyrosine kinase inhibitors [ Transl Oncol, 2023, 35:101712] PubMed: 37354638
Histone deacetylase 1 controls cardiomyocyte proliferation during embryonic heart development and cardiac regeneration in zebrafish [ PLoS Genet, 2021, 17(11):e1009890] PubMed: 34723970
Reduced Mitochondrial Apoptotic Priming Drives Resistance to BH3 Mimetics in Acute Myeloid Leukemia [ Cancer Cell, 2020, 38(6):872-890.e6] PubMed: 33217342
Lack of FGF21 promotes NASH-HCC transition via hepatocyte-TLR4-IL-17A signaling [ Theranostics, 2020, 10(22):9923-9936] PubMed: 32929325

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。