STM2457

製品コードS9870 バッチS987008

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

C25H28N6O2
分子量 444.53 CAS No. 2499663-01-1
Solubility (25°C)* 体外 DMSO 22 mg/mL (49.49 mM)
Ethanol 22 mg/mL (49.49 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5% DMSO 95% corn oil
0.4mg/ml 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. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
1.25mg/ml Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL 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 STM2457 is a highly potent and selective first-in-class catalytic inhibitor of RNA Methyltransferase METTL3 with an IC50 of 16.9 nM. STM2457 is highly specific for METTL3 and showed no inhibition of other RNA methyltransferases.
in vitro

STM2457 has a highly efficient and selective catalytic inhibition on RNA methyltransferase METTL3, causing gene-expression defects consistent with an effect on the mRNA translational efficiency of m6A substrates.[1]
in vivo

STM2457 prevents acute myeloid leukaemia (AML) expansion and reduces the number of key leukaemia stem cells in vivo.[1]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 MOLM-13 cells
濃度 0.1, 1, 5 and 10 μM
反応時間 --
実験の流れ

Western blot analysis
動物実験 動物モデル AML PDX-1 mice (NPM1c cells), AML PDX-2 mice (MLL-AF6 cells), AML PDX-3 mice (MLL-AF10)
投薬量 50 mg/kg
投与方法 --

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：

Suppression of the METTL3-m6A-integrin β1 axis by extracellular acidification impairs T cell infiltration and antitumor activity [ Cell Rep, 2024, 43(2):113796] PubMed: 38367240
M6A-modified circRBM33 promotes prostate cancer progression via PDHA1-mediated mitochondrial respiration regulation and presents a potential target for ARSI therapy [ Int J Biol Sci, 2023, 19(5):1543-1563] PubMed: 37056926
METTL3-mediated m6A modification of IGFBP7-OT promotes osteoarthritis progression by regulating the DNMT1/DNMT3a-IGFBP7 axis [ Cell Rep, 2023, 42(6):112589] PubMed: 37270777
m6A methyltransferase METTL3 programs CD4+ T-cell activation and effector T-cell differentiation in systemic lupus erythematosus [ Mol Med, 2023, 29(1):46] PubMed: 37013484
METTL3 exacerbates insulin resistance in hepatocytes by regulating m6A modification of cytochrome P450 2B6 [ Nutr Metab (Lond), 2023, 20(1):40] PubMed: 37710320
METTL3 exacerbates insulin resistance in hepatocytes by regulating m6A modification of cytochrome P450 2B6 [ Nutr Metab (Lond), 2023, 20(1):40] PubMed: 37710320
N6-methyladenosine modification governs liver glycogenesis by stabilizing the glycogen synthase 2 mRNA [ Nat Commun, 2022, 13(1):7038] PubMed: 36396934
METTL3 overexpression aggravates LPS-induced cellular inflammation in mouse intestinal epithelial cells and DSS-induced IBD in mice [ Cell Death Discov, 2022, 8(1):62] PubMed: 35165276
METTL3 inhibition reduces N6 -methyladenosine levels and prevents allogeneic CD4+ T-cell responses [ Immunol Cell Biol, 2022, 100(9):718-730] PubMed: 36005900

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。