| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C20H24N4O2S2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
LF3 is an antagonist of the β-catenin/TCF4 interaction with antitumor activity, showing an IC50 of 1.65 μM[1]. It is supplied as a white to off-white solid (C20H24N4O2S2, MW 416.56) at 99.55% purity.
Physical & Chemical Properties
| CAS Number | 664969-54-4 |
|---|---|
| Molecular Formula | C20H24N4O2S2 |
| Molecular Weight | 416.56 g/mol |
| Purity | 99.55% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | S=C(N1CCN(C/C=C/C2=CC=CC=C2)CC1)NC3=CC=C(S(=O)(N)=O)C=C3 |
| Signaling Pathway | Stem Cell/Wnt |
| Solubility | In Vitro: DMSO: 233.33 mg/mL (560.14 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
IC50: 1.65 μM (β-Catenin/TCF4, AlphaScreen), 1.82 μM (β-Catenin/TCF4, ELISA)[1]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 233.33 mg/mL (560.14 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (6.00 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.08 mg/mL (4.99 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.08 mg/mL (4.99 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 900 μL corn oil. |
Direct preparation of the working solution
These formulations are prepared directly, without a DMSO stock; use them promptly after preparation.
Protocol 4
| Composition | 0.5% CMC-Na/saline water |
|---|---|
| Result | 5 mg/mL (12.00 mM); suspension; requires sonication |
Data provided by the manufacturer.
In Vitro
LF3 inhibits Wnt/β-catenin signals in colon cancer cells with endogenously high Wnt activity and in cells carrying exogenous reporters. LF3 also suppresses Wnt signaling-related features of cancer cells, including high cell motility, cell-cycle progression, and overexpression of Wnt target genes. LF3 does not, however, cause cell death or interfere with cadherin-mediated cell-cell adhesion. Notably, LF3 blocks the self-renewal capacity of cancer stem cells in a concentration-dependent manner[1].
In Vivo
In a mouse xenograft model of colon cancer, LF3 reduces tumor growth and induces differentiation. Tumor growth is significantly reduced when mice bearing GFPhigh cells are treated with LF3 at 50 mg/kg. LF3 treatment leaves the normal histology of the mouse gut undisturbed[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Melatonin inhibits ESCC tumor growth by mitigating the HDAC7/β-catenin/c-Myc positive feedback loop and suppressing the USP10-maintained HDAC7 protein stability. Mil Med Res 2022 Sep 27;9(1):54. PMID: 36163081
Nuclear to Cytoplasmic Transport Is a Druggable Dependency in HDAC7-driven Small Cell Lung Cancer. Adv Sci (Weinh) 2025 Apr;12(14):e2413445. PMID: 39887933
Visible light-initiated radical 1,3-difunctionalization of β,γ-unsaturated ketones. Sci Adv 2022 Dec 9;8(49):eabq8596. PMID: 36490351
Dysregulated Wnt/β-catenin signaling confers resistance to cuproptosis in cancer cells. Cell Death Differ 2024 Nov;31(11):1452-1466. PMID: 38987382
Inhibition of neutrophil extracellular traps alleviates blood-brain barrier disruption and cognitive dysfunction via Wnt3/β-catenin/TCF4 signaling in sepsis-associated encephalopathy. J Neuroinflammation 2025 Mar 18;22(1):87. PMID: 40102948
Canonical Wnt signaling affects calcium homeostasis in serum-treated AC16 cells through MLN-mediated SERCA2a regulation. J Mol Cell Biol 2025 Dec 5:mjaf050. PMID: 41348974
Wnt/β-catenin pathway induces cardiac dysfunction via AKAP6-mediated RyR2 phosphorylation and sarcoplasmic reticulum calcium leakage. J Mol Cell Biol 2025 Jul 28;17(2):mjaf002. PMID: 40097291
Constitutive β-Catenin Overexpression Represses Lncrna MIR100HG Transcription via HDAC6-Mediated Histone Modification in Colorectal Cancer. Mol Cancer Res 2022 Jun 3;20(6):949-959. PMID: 35247921
YTHDF1-mediated mitochondrial dysfunction and allergic airway inflammation by interaction with β-catenin/TCF4 signaling. Int Immunopharmacol 2025 Sep 23:162:115181. PMID: 40633209
A deep tabular data learning model predicting cisplatin sensitivity identifies BCL2L1 dependency in cancer. Comput Struct Biotechnol J 2023 Jan 16:21:956-964. PMID: 36733702
