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 is a specific inhibitor of canonical Wnt signaling by disrupting the interaction between β-catenin and TCF4 with an IC50 less than 2 μM.
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[1].
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[1].

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。

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