LF3

Catalog No.S8474 Batch:S847401

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Technical Data

Formula

C20H24N4O2S2
Molecular Weight 416.56 CAS No. 664969-54-4
Solubility (25°C)* In vitro DMSO 83 mg/mL (199.25 mM)
Ethanol 5 mg/mL (12.0 mM)
Water Insoluble
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description 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.
Targets
β-catenin/Tcf4 [1]
(Cell-free assay)
1.65 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 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. LF3 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].

Protocol (from reference)

Cell Assay:[1]
  • Cell lines

    The cell lines HCT116, HCT15, HT29, SW480, SW620, LS174T, SW48, MCF7, HeLa, HEK293, and MDCK 

  • Concentrations

    3.3-60 μmol/L

  • Incubation Time

    24 h

  • Method

    β-catenin is immunoprecipitated from protein extracts of the cells that are incubated with LF3 at increasing concentrations, and reduced TCF4 and LEF1 bound to β-catenin are shown by Western blotting.
Animal Study:[1]
  • Animal Models

    NOD/SCID mice

  • Dosages

    50 mg/kg

  • Administration

    i.v.

Selleck's LF3 has been cited by 18 publications

Extrachromosomal circular DNA promotes prostate cancer progression through the FAM84B/CDKN1B/MYC/WWP1 axis [ Cell Mol Biol Lett, 2024, 29(1):103] PubMed: 38997648
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
Stromal-induced epithelial-mesenchymal transition induces targetable drug resistance in acute lymphoblastic leukemia [ Cell Rep, 2023, 42(7):112804] PubMed: 37453060
Wnt/beta-catenin signaling confers ferroptosis resistance by targeting GPX4 in gastric cancer [ Cell Death Differ, 2022, 10.1038/s41418-022-01008-w] PubMed: 35534546
Mechanosensitive Piezo1 is crucial for periosteal stem cell-mediated fracture healing [ Int J Biol Sci, 2022, 18(10):3961-3980] PubMed: 35844802

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.