Gambogenic acid

製品コードS9031 バッチS903103

印刷

化学情報

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

C38H46O8
分子量 630.77 CAS No. 173932-75-7
Solubility (25°C)* 体外 DMSO 100 mg/mL (158.53 mM)
 
 
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO Corn oil
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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 Gambogenic Acid, identified from Gamboge, is an inhibitor of the FGFR signaling pathway in erlotinib-resistant non-small-cell lung cancer (NSCLC) and exhibits anti-tumor effects. Gambogenic acid acts is also an effective inhibitor of EZH2 that specifically and covalently binds to Cys668 within the EZH2-SET domain, and triggers EZH2 ubiquitination.
in vitro

Gambogenic acid as a novel agent that specifically and covalently bound to Cys668 within the EZH2‐SET domain, triggers EZH2 degradation through COOH terminus of Hsp70‐interacting protein (CHIP)‐mediated ubiquitination. Gambogenic acid significantly suppresses H3K27Me3 and effectively reactivated polycomb repressor complex 2 (PRC2)‐silenced tumor suppressor genes. Gambogenic acid significantly suppresses tumor growth in an EZH2‐dependent manner.[1]
in vivo

In xenograft mouse model, gambogenic acid derivative GNA002 significantly decreases the volumes of Cal‐27‐derived tumors, and reduces H3K27Me3 levels in tumor tissues.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Head and neck cancer cell lines, humen breast cancer cell lines, mouse embryonic fibroblasts (MEFs)
濃度 0.2 -10 µM
反応時間 24 h, 48 h
実験の流れ

Cancer cells are treated with 2 μM GNA or GNA002 for 24 h. The cells are then harvested and re‐suspended with 500 μl of binding buffer. The cell suspension (100 μl) is incubated with various cell dye. The stained cells are analyzed with fluorescent‐activated cell sorting using the flow cytometry machine.
動物実験 動物モデル Nude mice bearing Cal‐27 xenograft tumors
投薬量 50 mg/kg
投与方法 p.o.

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：

Gambogenic acid induces cell death in human osteosarcoma through altering iron metabolism, disturbing the redox balance, and activating the P53 signaling pathway [ Chem Biol Interact, 2023, 382:110602] PubMed: 37302459
A high-content AlphaScreen™ identifies E6-specific small molecule inhibitors as potential therapeutics for HPV+ head and neck squamous cell carcinomas [ Oncotarget, 2021, 12(6):549-561] PubMed: 33796223
Targeting USP9x/SOX2 axis contributes to the anti-osteosarcoma effect of neogambogic acid. [ Cancer Lett, 2020, 469:277-286] PubMed: 31605775

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。