GPNA hydrochloride

製品コードS6670 バッチS667002

印刷

化学情報

 Chemical Structure Synonyms L-γ-Glutamyl-p-nitroanilide hydrochloride Storage
(From the date of receipt)
3 years -20°C powder
化学式

C11H14ClN3O5

分子量 303.7 CAS No. 67953-08-6
Solubility (25°C)* 体外 DMSO 5 mg/mL (16.46 mM)
Water Insoluble
Ethanol 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。

0.250mg/ml (0.82mM) Taking the 1 mL working solution as an example, add 50 μL of 5 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. 
Clear solution
5% DMSO 95% Corn oil

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。

0.250mg/ml (0.82mM) Taking the 1 mL working solution as an example, add 50 μL of 5 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 GPNA hydrochloride (L-γ-glutamyl-p-nitroanilide hydrochloride) is a substrate of γ-glutamyltransferase (GGT) and an inhibitor of the glutamine transporter ASCT2 with an IC50 of ~250 μM in A549 cells. It also inhibits Na+-dependent carriers SNAT1, -2, -4, -5 and Na+-independent leucine transporters LAT1/2. It can be widely used in research on pancreatic cancer, breast cancer, glioblastoma multiforme, acute myelogenous leukemia, and non-small-cell lung cancer.
in vitro

GPNA leads to a significant decrease in endometrial cancer cell growth and spheroid cross-sectional area.[1]

in vivo

EGFRAS-GPNA (EGFRAS-specific GPNA oligomers) is taken-up by several tissues including the xenograft tumor. Systemic administration of EGFRAS-GPNA induces antitumor effects in HNSCC xenografts, with similar efficacies as the FDA-approved EGFR inhibitors: cetuximab and erlotinib. EGFRAS-GPNA effectively againsts the constitutively active EGFR vIII mutant implicated in cetuximab resistance.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Endometrial cancer cell line
濃度 1 mM
反応時間 24 h
実験の流れ

Cells (1–2 × 105) are cultured for 24 h followed by treatment where stated with vehicle or 1 mm GPNA for 24 h. And then staining for flow cytometric analysis is performed. MTT assays are conducted using 100–250 cells per well in a 96-well plate. Fresh media with vehicle or 1 mm GPNA are applied every two days.

動物実験 動物モデル HNSCC xenograft-bearing nude mice
投薬量 5 mg/kg
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/30696905/

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:

Cooperative nutrient scavenging is an evolutionary advantage in cancer [ Nature, 2025, 10.1038/s41586-025-08588-w] PubMed: 39972131
Androgens drive SLC1A5-dependent metabolic reprogramming in polycystic ovary syndrome [ Nat Commun, 2025, 16(1):7611] PubMed: 40817119
Lipophagy-mediated cholesterol synthesis inhibition is required for the survival of hepatocellular carcinoma under glutamine deprivation [ Redox Biol, 2023, 63:102732] PubMed: 37150151
Inhibition of SND1 overcomes chemoresistance in bladder cancer cells by promoting ferroptosis [ Oncol Rep, 2023, 49(1)16] PubMed: 36453257
Neddylation inhibition induces glutamine uptake and metabolism by targeting CRL3SPOP E3 ligase in cancer cells [ Nat Commun, 2022, 13(1):3034] PubMed: 35641493
Antagonizing Glutamine Bioavailability Promotes Radiation Sensitivity in Prostate Cancer [ Cancers (Basel), 2022, 14(10)2491] PubMed: 35626095
Evaluation of Glutaminolysis in T Cells [ Curr Protoc, 2022, 2(9):e540] PubMed: 36111948

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。