Piperlongumine

製品コードS7551 バッチS755105

印刷

化学情報

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

C17H19NO5
分子量 317.34 CAS No. 20069-09-4
Solubility (25°C)* 体外 DMSO 63 mg/mL warmed with 50ºC water bath (198.52 mM)
Ethanol 63 mg/mL warmed with 50ºC water bath (198.52 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 Piperlongumine (PPLGM, Piplartine), a natural alkaloid from Piper longum L., increases the level of reactive oxygen species (ROS) and selectively kills cancer cells. It is a direct TrxR1 inhibitor with suppressive activity against gastric cancer and a novel inhibitor of CRM1; also an inhibitor of PI3K/Akt/mTOR in human breast cancer cells.
in vitro Piperlongumine is a known ROS inducer which could induce pancreatic cancer cell death in cell culture[1] As a thromboxane A(2) receptor antagonist, Piperlongumine inhibits platelet aggregation. [2] Piperlongumine also promotes autophagy via inhibition of Akt/mTOR signalling and mediates cancer cell death. [3]
in vivo Piperlongumine (50 mg/kg i.p.) causes in vivo growth inhibition of tumor cells without leading to major changes in the biochemical, hematological and histopathological parameters. [4]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 MCF-7 and 786-O cells
濃度 ~10 μM
反応時間 48 hours
実験の流れ

MCF-7 and 786-O cells are incubated with various PL concentrations for 48h. Cell proliferation is analysed by CellTiter Blue assay. Effective doses (ED) are calculated using XLift, Microsoft Excel add-in.
動物実験 動物モデル Mice transplanted with sarcoma 180 tumors
投薬量 ~50 mg/kg
投与方法 i.p.

カスタマーフィードバック

Data from [Data independently produced by , , Oncotarget, 2016, 7(35):56933-56943]

Data from [Data independently produced by , , Oncotarget, 2016, 7(26):40531-40545]

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：

Piperlongumine conquers temozolomide chemoradiotherapy resistance to achieve immune cure in refractory glioblastoma via boosting oxidative stress-inflamation-CD8+-T cell immunity [ J Exp Clin Cancer Res, 2023, 42(1):118] PubMed: 37161450
Identification of Piperlongumine as Potent Inhibitor of Necroptosis [ Drug Des Devel Ther, 2023, 17:1387-1394] PubMed: 37188283
Grainyhead 1 acts as a drug-inducible conserved transcriptional regulator linked to insulin signaling and lifespan [ Nat Commun, 2022, 13(1):107] PubMed: 35013237
USP5-Beclin 1 axis overrides p53-dependent senescence and drives Kras-induced tumorigenicity [ Nat Commun, 2022, 13(1):7799] PubMed: 36528652
Systematic identification of biomarker-driven drug combinations to overcome resistance [ Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7] PubMed: 35332332
Screening Health-Promoting Compounds for Their Capacity to Induce the Activity of FOXO3 [ J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493] PubMed: 34508571
A "Failed" Assay Development for the Discovery of Rescuing Small Molecules from the Radiation Damage [ SLAS Discov, 2021, 24725552211020678] PubMed: 34151632
MLH1 Deficiency Induces Cetuximab Resistance in Colon Cancer via Her-2/PI3K/AKT Signaling [ Adv Sci (Weinh), 2020, 7(13):2000112] PubMed: 32670759
Engineering Chromosome Region Maintenance 1 Fragments That Bind to Nuclear Export Signals [ Protein Sci, 2020, 29(6):1366-1372] PubMed: 31495993
Inhibition of ERKs/Akt-Mediated c-Fos Expression Is Required for Piperlongumine-Induced Cyclin D1 Downregulation and Tumor Suppression in Colorectal Cancer Cells [ Onco Targets Ther, 2020, 13:5591-5603] PubMed: 32606774

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。