RIN1 (RBPJ Inhibitor-1)

製品コードS3376 バッチS337601

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

C17H14FN3O2

分子量 311.31 CAS No. 2682114-39-0
Solubility (25°C)* 体外 DMSO 62 mg/mL (199.15 mM)
Ethanol 62 mg/mL (199.15 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。

0.300mg/ml (0.96mM) Taking the 1 mL working solution as an example, add 50 μL of 6 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. 
* <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 RIN1 (RBPJ Inhibitor-1) is a potent inhibitor of the transcription factor RBPJ that disrupts the interaction between NOTCH and RBPJ.
in vitro

RIN1 (RBPJ Inhibitor-1) blocks the functional interaction of RBPJ with SHARP, a scaffold protein that forms a transcriptional repressor complex with RBPJ in the absence of NOTCH signaling. Consistent with disruption of NOTCH signaling, this compound inhibits the proliferation of hematologic cancer cell lines and promotes skeletal muscle differentiation from C2C12 myoblasts.[1]

in vivo

RIN1 (RBPJ Inhibitor-1) is a potent inhibitor of the transcription factor RBPJ that disrupts the interaction between NOTCH and RBPJ.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 AD-293 cells
濃度 2 µM
反応時間 17 h
実験の流れ

AD-293 cells were transfected with RBPJ-VP16myc and 48 hours later were treated±RIN1 (RBPJ Inhibitor-1, 2 µM), Cycloheximide (CHX, 10 µg/ml) for an additional 17 hours and then assayed for Hes1-Luciferase activity.

動物実験 動物モデル BALB/c-nude mice
投薬量 40 mg/kg
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/31346210/
  • https://pubmed.ncbi.nlm.nih.gov/35368029/

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:

CD69+CD103+CD8+ tissue-resident memory T cells possess stronger anti-tumor activity and predict better prognosis in colorectal cancer [ Cell Commun Signal, 2024, 22(1):608] PubMed: 39696312
Polycomb Repressive Complex 2 promotes atherosclerotic plaque vulnerability [ bioRxiv, 2024, 2024.12.02.626505] PubMed: 39703699
Endothelial γ-protocadherins inhibit KLF2 and KLF4 to promote atherosclerosis [ Nat Cardiovasc Res, 2024, 3(9):1035-1048] PubMed: 39232138
Evaluation of the anticancer activity of RIN-1, a Notch signaling modulator, in head and neck squamous cell carcinoma [ Sci Rep, 2023, 13(1):13700] PubMed: 37607974
Characterisation of the Notch signalling small molecule inhibitor RIN1 [ University of Zagreb Faculty of Science, 2023, ] PubMed: None
Regulation of reverse electron transfer at mitochondrial complex I by unconventional Notch action in cancer stem cells [ Dev Cell, 2022, 57(2):260-276.e9] PubMed: 35077680

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。