MS049

製品コードS8147 バッチS814701

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

C15H26Cl2N2O

分子量 321.29 CAS No. 2095432-59-8
Solubility (25°C)* 体外 DMSO 56 mg/mL (174.29 mM)
Water 56 mg/mL (174.29 mM)
Ethanol 50 mg/mL (155.62 mM)
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。

2.8mg/ml (8.71mM) Taking the 1 mL working solution as an example, add 50 μL of 56 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。

0.4mg/ml (1.24mM) Taking the 1 mL working solution as an example, add 50 μL of 8 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 MS049 is a potent and selective inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively.
in vitro MS049 does not inhibit any of the methyltransferases at 50 μM or demethylases at 10 μM and does not display appreciable binding to any of the methyllysine/methylarginine reader proteins using the DSF assay at 200 μM. This compound demonstrated excellent selectivity over a broad range of epigenetic and nonepigenetic targets. In cellular assays, it potently inhibits the methyltransferase activity of PRMT4 and PRMT6 and reduces levels of Med12me2a and H3R2me2a in HEK293 cells[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HEK293 cells
濃度 0, 1, 10, and 50 μM
反応時間 96 h
実験の流れ

HEK293 cells grown in DMEM supplemented with 10% FBS, penicillin (100 U/mL), and streptomycin (100 μg/mL) were seeded on 96-well plates at density 3000/well and treated with this compound at 0, 1, 10, and 50 μM concentrations for 96 h. The confluency was measured using IncuCyte ZOOM live cell imaging device and analyzed with IncuCyte ZOOM software based on phase contrast images.

参考

  • https://pubmed.ncbi.nlm.nih.gov/27584694/

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:

PRMT6-mediated ADMA promotes p62 phase separation to form a negative feedback loop in ferroptosis [ Theranostics, 2024, 14(10):4090-4106] PubMed: 38994016
Hypoxia Stimulates SUMOylation-Dependent Stabilization of KDM5B [ Front Cell Dev Biol, 2021, 9:741736] PubMed: 34977006
Hypoxia stimulates SUMOylation-dependent stabilization of KDM5B [ Research Square, 2021, 10.21203/rs.3.rs-620216/v1] PubMed: None
Arginine Methylation-Dependent LSD1 Stability Promotes Invasion and Metastasis of Breast Cancer [ EMBO Rep, 2020, 21(2):e48597] PubMed: 31833203

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。