VH298

製品コードS8449 バッチS844901

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

C27H33N5O4S

分子量 523.65 CAS No. 2097381-85-4
Solubility (25°C)* 体外 DMSO 100 mg/mL (190.96 mM)
Ethanol 100 mg/mL (190.96 mM)
Water 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。

5.000mg/ml (9.55mM) Taking the 1 mL working solution as an example, add 50 μL of 100 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。

0.625mg/ml (1.19mM) Taking the 1 mL working solution as an example, add 50 μL of 12.5 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 VH298 is a potent VHL (Von Hippel-Lindau, the E3 ligase) inhibitor that stabilizes HIF-α. VH298 blocks the VHL:HIF-α interaction with Kd of 90 nM in isothermal titration calorimetry (ITC) and 80 nM in a competitive fluorescence polarization assay. VH-298 can be used in PROTAC technology.
in vitro

VH298 can activate the HIF-1 signalling pathway by stabilizing both forms of HIF-1α in vitro. This compound promotes rFb variability, migration, and synthesis of collagen and regulatory cell factors. It improves the angiogenesis of hUVEC.[2]

in vivo

VH298 can activate the HIF-1 signalling pathway by stabilizing both forms of HIF-1α in vitro. This compound promotes rFb variability, migration, and synthesis of collagen and regulatory cell factors. It improves the angiogenesis of hUVEC.[2]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 rFb cells, hUVEC cells
濃度 10 μM, 30 μM, 100 μM, 200 μM
反応時間 48 h
実験の流れ

The rFb are trypsinised and placed in flat-bottomed 96-well plates at an initial density of 5000 cells per well. After 24 h of incubation, the medium is changed to VH298-containing medium at different dosages (0 μM, 10 μM, 30 μM, 100 μM, and 200 μM). rFb are incubated at 37°C for 48 h. The proliferation is determined by the Cell Counting Kit-8 (CCK-8) assay. After incubation, rFb are treated with the CCK-8 solution at a final concentration of 10% for 2 h at 37°C, followed by measurement of absorbance at 450nm using a microplate reader.

動物実験 動物モデル Sprague-Dawley rats intraperitoneal injected of streptozotocin at 65 mg/kg
投薬量 30 μM VH298 in PBS (100 microlitres)
投与方法 local injection

参考

  • https://pubmed.ncbi.nlm.nih.gov/27811928/
  • https://pubmed.ncbi.nlm.nih.gov/30911550/

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:

Distinct TAM subset with cross-dressing capability determines the bifurcation of tumor immunity [ Cell Rep, 2025, 44(6):115800] PubMed: 40489329
Lactylation modification of HIF-1α enhances its stability by blocking VHL recognition [ Cell Commun Signal, 2025, 23(1):364] PubMed: 40760493
Design, synthesis, and biological evaluation of first-in-class indomethacin-based PROTACs degrading SARS-CoV-2 main protease and with broad-spectrum antiviral activity [ Eur J Med Chem, 2024, 268:116202] PubMed: 38394929

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。