6-Diazo-5-oxo-L-norleucine

製品コードS8620 バッチS862002

印刷

化学情報

 Chemical Structure Synonyms Diazooxonorleucine, 6-Diazo-5-oxo-L-nor-Leucine, L-6-Diazo-5-oxonorleucine, DON Storage
(From the date of receipt)
3 years -20°C powder
化学式

C6H9N3O3

分子量 171.15 CAS No. 157-03-9
Solubility (25°C)* 体外 Water 34 mg/mL (198.65 mM)
DMSO Insoluble
Ethanol 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 6-Diazo-5-oxo-L-norleucine (Diazooxonorleucine, L-6-Diazo-5-oxonorleucine, DON), an antibiotic isolated from Streptomyces, is a glutaminase antagonist with IC50 of ~1  mM for cKGA (kidney-type glutaminase). 6-Diazo-5-oxo-L-norleucine exhibits analgesic, antibacterial, antiviral and anticancer properties.
in vitro

6-Diazo-5-oxo-L-norleucine appears to be positive in the in vitro chromosome aberration assay that it demonstrates dose dependent statistically positive increase in structural aberrations at 4 and 20 hour exposure without S9 and also at 4 hour exposure with S9.[2]

in vivo

6-Diazo-5-oxo-L-norleucine is evaluated for its in vivo clastogenic activity by detecting micronuclei in polychromatic erythrocyte (PCE) cells in bone marrow collected from the male mice dosed intravenously with 500, 100, 10, 1 and 0.1 mg/kg at 24 and 48 hour post dose. The in vivo micronucleus assay reveals a statistically positive response for micronucleus formation at 500, 100 and 10 mg/kg at 24 and 48 hour post dose.[2]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Chinese hamster ovary (CHO) cells
濃度 0.1712 μg/mL to 1712 μg/mL
反応時間 4 h, 20 h
実験の流れ

CHO cells are exposed to vehicle alone and to nine dose levels of test article, ranging from 0.1712 to 1712 μg/mL in the absence or presence of an S9 reaction mixture.

動物実験 動物モデル 6-week-old male ICR mice
投薬量 500 mg/kg, 100 mg/kg, 10 mg/kg, 1 mg/kg, 0.1 mg/kg
投与方法 IV

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:

Mitochondrial transplantation ameliorates doxorubicin-induced cardiac dysfunction via activating glutamine metabolism [ iScience, 2023, 26(10):107790] PubMed: 37731615
Increased glucose metabolism in TAMs fuels O-GlcNAcylation of lysosomal Cathepsin B to promote cancer metastasis and chemoresistance [ Cancer Cell, 2022, 40(10):1207-1222.e10] PubMed: 36084651
Glutamine Metabolism Is Required for Alveolar Regeneration during Lung Injury [ Biomolecules, 2022, 12(5)728] PubMed: 35625656
NDRG2 inhibits pyruvate carboxylase-mediated anaplerosis and combines with glutamine blockade to inhibit the proliferation of glioma cells [ Am J Cancer Res, 2022, 12(8):3729-3744] PubMed: 36119843
Inhibitory Effect of a Glutamine Antagonist on Proliferation and Migration of VSMCs via Simultaneous Attenuation of Glycolysis and Oxidative Phosphorylation [ Int J Mol Sci, 2021, 22(11)5602] PubMed: 34070527
Glutamine metabolism is essential for the production of IL-17A in γδ T cells and skin inflammation [ Tissue Cell, 2021, 71:101569] PubMed: 34146944
Oxidative phosphorylation safeguards pluripotency via UDP-N-acetylglucosamine [ bioRxiv, 2021, 10.1101/2021.07.06.451381] PubMed: None

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。