Tenovin-1

製品コードS8000 バッチS800001

印刷

化学情報

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

C20H23N3O2S

分子量 369.48 CAS No. 380315-80-0
Solubility (25°C)* 体外 DMSO 250 mg/mL (676.62 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.
Homogeneous suspension
15% Captisol

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。

10.000mg/ml (27.07mM) Taking the 1 mL working solution as an example, take 10 mg of this product, add it to 1 ml of 15% Captisol clear solution, and mix evenly to form a uniform suspension. 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 Tenovin-1 protects against MDM2-mediated p53 degradation, which involves ubiquitination, and acts through inhibition of protein-deacetylating activities of SirT1 and SirT2. Tenovin-1 is also an inhibitor of dihydroorotate dehydrogenase (DHODH).
in vitro

Tenovin-1 is a p53 activator and elevates the amount of p53 protein within 2 hr of treatment. This compound treatment does not alter p53 mRNA levels. It (10μM) protects p53 from mdm2-mediated degradation with little effect on p53 synthesis. This chemical represses cell growth, and induces apoptosis in a panel of tumor cells expressing p53. It acts through inhibition of the protein-deacetylating activities of SirT1 and SirT2, two important members of the sirtuin family. [1]

in vivo

Initial in vivo experiments indicated that tenovin-1 impairs the growth of BL2-derived tumor xenografts. [1]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HCT116, HCT116 p53−/−, EW36, BL2, NTera2D, NTera2D-DNp53, ARN8, NHDF, SKNH-pCMV and SKNSH-DNp53.
濃度 10 μM
反応時間 4 days
実験の流れ

Cell viability is determined by trypan blue exclusion, Giemsa staining, or MTT assays.

動物実験 動物モデル Female SCID mice injected subcutaneously with ARN8 cells suspended in matrigel.
投薬量 92.5 mg/kg
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/18455128/
  • https://pubmed.ncbi.nlm.nih.gov/32900849/

カスタマーフィードバック

Data from [Data independently produced by , , Journal of Functional Foods, 2018, 40:544-553]

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:

How hydrophilic group affects drug-protein binding modes: Differences in interaction between sirtuins inhibitors Tenovin-1/Tenovin-6 and human serum albumin [ J Pharm Biomed Anal, 2021, 201:114121] PubMed: 34020341
Circular RNA hsa_circ_0055538 regulates the malignant biological behavior of oral squamous cell carcinoma through the p53/Bcl-2/caspase signaling pathway. [ J Transl Med, 2019, 17(1):76] PubMed: 30857544
Increased expression of Sonic hedgehog restores diabetic endothelial progenitor cells and improves cardiac repair after acute myocardial infarction in diabetic mice. [ Int J Mol Med, 2019, 44(3):1091-1105] PubMed: 31524224
DRUGPATH - a novel bioinformatic approach identifies DNA-damage pathway as a regulator of size maintenance in human ESCs and iPSCs [ Sci Rep, 2019, 9(1):1897] PubMed: 30760778
The protective effect of PFTα on alcohol-induced osteonecrosis of the femoral head [ Oncotarget, 2017, 8(59):100691-100707] PubMed: 29246013
The protective effect of PFTα on alcohol-induced osteonecrosis of the femoral head [ Oncotarget, 2017, 8(59):100691-100707] PubMed: 29246013

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。