LF3

製品コードS8474 バッチS847402

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

C20H24N4O2S2

分子量 416.56 CAS No. 664969-54-4
Solubility (25°C)* 体外 DMSO 83 mg/mL (199.25 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.
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。

4.150mg/ml (9.96mM) Taking the 1 mL working solution as an example, add 50 μL 83 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 LF3は、β-カテニンとTCF4の相互作用を阻害することにより、canonical Wntシグナル伝達を特異的に阻害する阻害剤であり、IC50は2 μM未満です。
in vitro LF3 does not cause cell death or interfere with cadherin-mediated cell-cell adhesion. The self-renewal capacity of cancer stem cells is blocked by this compound in concentration-dependent manners, as examined by sphere formation of colon and head and neck cancer stem cells under nonadherent conditions. It inhibits Wnt/β-catenin signaling, but does not interfere with E-cadherin/β-catenin-mediated cell-cell adhesion. This chemical blocks the expression of a series of Wnt target genes in Wnt-addicted colon cancer cells. It inhibits proliferation of Wnt-addicted colon cancer cells through induction of cell-cycle arrest and also inhibits self-renewal capacity of CSCs.
in vivo LF3 reduces tumor growth and induces differentiation in a mouse xenograft model of colon cancer while exhibiting no significant toxicity for mice and does not disturb the normal histology of the gut of mice.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 The cell lines HCT116, HCT15, HT29, SW480, SW620, LS174T, SW48, MCF7, HeLa, HEK293, and MDCK 
濃度 3.3-60 μmol/L
反応時間 24 h
実験の流れ β-catenin is immunoprecipitated from protein extracts of the cells that are incubated with this compound at increasing concentrations, and reduced TCF4 and LEF1 bound to β-catenin are shown by Western blotting.
動物実験 動物モデル NOD/SCID mice
投薬量 50 mg/kg
投与方法 i.v.

参考

  • https://pubmed.ncbi.nlm.nih.gov/26645562/

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:

Biomimetic nanocrystals co-deliver paclitaxel and small-molecule LF3 for ferroptosis-combined chemotherapy for gastric cancer [ Colloids Surf B Biointerfaces, 2025, 251:114586] PubMed: 40010081
Extrachromosomal circular DNA promotes prostate cancer progression through the FAM84B/CDKN1B/MYC/WWP1 axis [ Cell Mol Biol Lett, 2024, 29(1):103] PubMed: 38997648
Key epigenetic and signaling factors in the formation and maintenance of the blood-brain barrier [ Elife, 2024, 12RP86978] PubMed: 39670988
Sphingosylphosphorylcholine Promotes Th9 Cell Differentiation Through Regulation of Smad3, STAT5, and β-Catenin Pathways [ Immune Netw, 2024, 24(6):e45] PubMed: 39801737
Functional analysis of a first hindlimb positioning enhancer via Gdf11 expression [ Front Cell Dev Biol, 2024, 12:1302141] PubMed: 38559809
Mice with renal-specific alterations of stem cell-associated signaling develop symptoms of chronic kidney disease but surprisingly no tumors [ PLoS One, 2024, 19(3):e0282938] PubMed: 38512983
Single-cell RNA sequencing of intestinal crypts reveals vital events in damage repair and the double-edged sword effect of the Wnt3/β-catenin pathway in irradiated mice [ Redox Biol, 2023, 10.1016/j.redox.2023.102942] PubMed: 37918127
Single-cell RNA sequencing of intestinal crypts reveals vital events in damage repair and the double-edged sword effect of the Wnt3/β-catenin pathway in irradiated mice [ Redox Biol, 2023, 68:102942.] PubMed: 37918127
Oridonin promotes endoplasmic reticulum stress via TP53-repressed TCF4 transactivation in colorectal cancer [ J Exp Clin Cancer Res, 2023, 42(1):150] PubMed: 37337284
Attenuation of amyloid-β-induced mitochondrial dysfunction by active components of anthocyanins in HT22 neuronal cells [ MedComm (2020), 2023, 4(4):e301] PubMed: 37346934

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。