LF3 Wnt/beta-catenin inhibitor

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.

LF3 Wnt/beta-catenin inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 416.56

Purity & Quality Control

Related Products

Mechanism of Action

Targets
β-catenin/Tcf4 [1]
(Cell-free assay)
1.65 μM

In vitro

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 this compound in concentration-dependent manners, as examined by sphere formation of colon and head and neck cancer stem cells under nonadherent conditions. It inhibits Wnt/β-catenin signaling, but does not interfere with E-cadherin/β-catenin-mediated cell-cell adhesion. This chemical 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].
Cell Research 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 this compound at increasing concentrations, and reduced TCF4 and LEF1 bound to β-catenin are shown by Western blotting.

In Vivo

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].
Animal Research Animal Models NOD/SCID mice
Dosages 50 mg/kg
Administration i.v.

References

  • https://pubmed.ncbi.nlm.nih.gov/26645562/

Chemical Information

Molecular Weight 416.56 Formula

C20H24N4O2S2

CAS No. 664969-54-4 SDF Download SDF
Synonyms N/A
Smiles C1CN(CCN1CC=CC2=CC=CC=C2)C(=S)NC3=CC=C(C=C3)S(=O)(=O)N

Storage and Stability

Storage (From the date of receipt)

In vitro
Batch:

DMSO : 83 mg/mL ( (199.25 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.