product name LF3
Description: LF3 is a specific antagonist of the β-Catenin/TCF4 interaction with antitumor activity; it has 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.
416.56
Formula
C20H24N4O2S2
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)
Solubility (In vivo)
Synonyms
other peoduct :
| 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: 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 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. |
| Animal model | NOD/SCID mice |
| Formulation & Dosage | 50 mg/kg; i.v. injection |
| References | Cancer Res. 2016 Feb 15;76(4):891-901. |
