(-)-Parthenolide

製品コードS2341 バッチS234106

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 49 mg/mL (197.32 mM)
Ethanol 49 mg/mL warmed with 50ºC water bath (197.32 mM)
Water Insoluble
* <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 (-)-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.
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]

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]

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 --

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:

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
Parthenolide inhibits ubiquitin-specific peptidase 7 (USP7), Wnt signaling, and colorectal cancer cell growth. [ J Biol Chem, 2020, 295(11):3576-3589] PubMed: 32029476
Parthenolide Inhibits Angiogenesis in Esophageal Squamous Cell Carcinoma Through Suppression of VEGF [ Onco Targets Ther, 2020, 13:7447-7458] PubMed: 32801767
Loss of N-Glycanase 1 Alters Transcriptional and Translational Regulation in K562 Cell Lines [ G3 (Bethesda), 2020, 4;10(5):1585-1597] PubMed: 32265286
An antiviral drug screening system for enterovirus 71 based on an improved plaque assay: A potential high-throughput method [ J Med Virol, 2019, 91(8):1440-1447] PubMed: 30900754
SIRT3 deacetylase activity confers chemoresistance in AML via regulation of mitochondrial oxidative phosphorylation. [ Br J Haematol, 2019, 187(1):49-64] PubMed: 31236919
Novel Targeted Nano-Parthenolide Molecule against NF-kB in Acute Myeloid Leukemia. [ Molecules, 2019, 24(11)] PubMed: 31163672

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。

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