LF3

SKU: orb1224300

Description

A small-molecule antagonist of the β-catenin/TCF4 interaction with IC50 of 1.65 and 1.82 uM in AlphaScreen and ELISA assay, respectively; potently and selectively inhibits activated Wnt/β-catenin signals in reporter cells (IC50=2.4-4 uM), does not cause cell death and interfere with the interaction of β-catenin with E-cadherin; reduces tumor growth and induces differentiation in a mouse xenograft model of colon cancer.

Key Properties

• CAS Number: 664969-54-4
• MW: 416.56016
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₄N₄O₂S₂
• SMILES: S=C(N1CCN(C/C=C/C2=CC=CC=C2)CC1)NC3=CC=C(S(=O)(N)=O)C=C3
• Target: Beta-catenin
• Solubility: DMSO: ≥ 32 mg/mL

Bioactivity

• In Vivo:
  LF3 reduces tumor growth and induces differentiation in a mouse xenograft model of colon cancer. Tumor growth is significantly reduced when mice with GFPhigh cells are treated with LF3 at 50 mg/kg. LF3 treatment does not disturb the normal histology of the gut of mice.
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• In Vitro:
  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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

LF-3 | LF 3

Quick Database Links

Gene Symbol

Beta-catenin