5-Iodotubercidin

製品コードS8314 バッチS831402

印刷

化学情報

Chemical Structure Synonyms NSC 113939, 5-ITu Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C11H13IN4O4
分子量 392.15 CAS No. 24386-93-4
Solubility (25°C)* 体外 DMSO 78 mg/mL (198.9 mM)
Water 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 5-Iodotubercidin (NSC 113939, 5-ITu) is a potent adenosine kinase inhibitor with IC50 of 26 nM. It inhibits nucleoside transporter, CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2 and PKC.
in vitro 5-Iodotubercidin(Itu) is a genotoxic drug that activates the Atm-p53 pathway and has anti-tumor activity. Itu is unique compared to other nucleoside analogs in the way that it induces G2 arrest in a p53 -dependent manner. Moreover, at higher doses, Itu might activate p53-independent pathways, which may cooperate with p53 to kill cells and inhibit tumor growth. Incorporation of Itu metabolite into DNA causes DNA breaks, which triggers the DNA damage response. Itu might be a potential chemotherapeutic drug with distinct working mechanisms[2].
in vivo 5-Iodotubercidin is a potent inhibitor of adenosine kinase in the rat brain. 5-iodotubercidin has potent hypotensive, muscle relaxant, and hypothermic actions in mice, and that these effects could be blocked by theophylline, an adenosine receptor antagonist. 5-iodotubercidin (1 mg/kg, i.p.) administered prior to an ischemic episode, fails to provide a degree of cerebroprotection, assessed either by locomotor or histopathological indices Even though 5-iodotubercidin administration is known to enhance extracellular adenosine levels in brain slices[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 The primary mouse embryo fibroblast (MEF) cells
濃度
反応時間 24 h or 48 h
実験の流れ Cells are seeded on 35-mm dishes and cultured for 24 hrs, reaching 60–70% confluency. The cells are treated with different concentrations of Itu for 24 or 48 hrs, harvested by trypsinization, resuspended in 200 µl PBS, and fixed in 100% ethanol overnight at 4°C. The fixed cells are pelleted by centrifugation, resuspended in 800 µl PBS containing ribonuclease A (100 µg/ml) and incubated for 30 min at 37°C. Then 10 µl propidium iodide (PI, 4 mg/ml PBS) are added to the samples, which are assessed on a FACSCalibur flow cytometer using Cell Quest software.
動物実験 動物モデル Male Mongolian gerbils
投薬量 1, 2.5 and 5 mg/kg
投与方法 i.p.

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：

Dihydronicotinamide Riboside Is a Potent NAD+ Precursor Promoting a Pro-Inflammatory Phenotype in Macrophages [ Front Immunol, 2022, 13:840246] PubMed: 35281060
Identification of New Vulnerabilities in Conjunctival Melanoma Using Image-Based High Content Drug Screening [ Cancers (Basel), 2022, 14(6)1575] PubMed: 35326726
Protein Kinase D-Dependent Downregulation Of Immediate Early Genes Through Class IIa Histone Deacetylases In Acute Lymphoblastic Leukemia [ Mol Cancer Res, 2021, molcanres.0808.2020] PubMed: 33980612
Genome-wide CRISPR screen uncovers a synergistic effect of combining Haspin and Aurora kinase B inhibition. [ Oncogene, 2020, 16] PubMed: 32300176

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。