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    LF3
    LF3

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V2725
    CAS #: 664969-54-4Purity ≥98%

    Description: LF3 is a specific antagonist of the β-Catenin/TCF4 interaction with antitumor activity; it acts by disrupting the interaction between β-catenin and TCF4 with an IC50 of 1.65 μM. 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 LF3 in concentration-dependent manners, as examined by sphere formation of colon and head and neck cancer stem cells under nonadherent conditions. LF3 inhibits Wnt/β-catenin signaling, but does not interfere with E-cadherin/β-catenin-mediated cell-cell adhesion. 

    References: Cancer Res. 2016 Feb 15;76(4):891-901.


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    Molecular Weight (MW)416.56
    FormulaC20H24N4O2S2
    CAS No.664969-54-4
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 83 mg/mL (199.3 mM)
    Water: <1 mg/mL
    Ethanol: 5 mg/mL (12.0 mM)
    SMILES Code S=C(N1CCN(C/C=C/C2=CC=CC=C2)CC1)NC3=CC=C(S(=O)(N)=O)C=C3
    Synonyms LF-3; LF 3


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    In Vitro

    In vitro activity: LF3 inhibits Wnt/β-catenin signals in cells with exogenous reporters and in colon cancer cells with endogenously high Wnt activity. LF3 also suppresses features of cancer cells related to Wnt signaling, including high cell motility, cell-cycle progression, and the overexpression of Wnt target genes. However, LF3 does not cause cell death or interfere with cadherin-mediated cell-cell adhesion. Remarkably, the self-renewal capacity of cancer stem cells is blocked by LF3 in concentration-dependent manners.


    Kinase Assay: LF3 has an IC50 of 1.65 μM (β-Catenin/TCF4, AlphaScreen), and 1.82 μM (β-Catenin/TCF4, ELISA).


    Cell Assay: LF3 is dissolved in DMSO to a concentration of 50 mM and diluted with culture medium. Two colon cancer cell lines (HCT116 and HT29) and a breast cancer cell line (MCF7) are treated with LF3 (0, 30, 60 μM) for 24 hours and labeled with BrdUrd for 4 to 5 hours to detect proliferating cells.

    In VivoLF3 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. 
    Animal modelNOD/SCID mice 
    Formulation & Dosage50 mg/kg; i.v. injection 
    ReferencesCancer Res. 2016 Feb 15;76(4):891-901.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    LF3

    Compound LF3 disrupts the interaction between β-catenin and TCF4. Cancer Res. 2016 Feb 15;76(4):891-901.
     

    LF3

    LF3 specifically inhibits Wnt/β-catenin signaling in cells. Cancer Res. 2016 Feb 15;76(4):891-901.
     

    LF3

    LF3 inhibits Wnt/β-catenin signaling in colon cancer cells. Cancer Res. 2016 Feb 15;76(4):891-901.
     

    LF3

    LF3 inhibits the self-renewal of colon CSCs. Cancer Res. 2016 Feb 15;76(4):891-901.
     

    LF3

    LF3 induces differentiation of mouse salivary gland CSCs. Cancer Res. 2016 Feb 15;76(4):891-901.
     

    LF3

    LF3 reduces tumor growth and induces differentiation of colon CSCs in vivo. Cancer Res. 2016 Feb 15;76(4):891-901.


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