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B-Catenin/Tcf Protein-Protein Interaction FP Assay


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Catalog No.:  K-5900

Description:  The K-5900 kit has been discontinued. Please contact Echelon in individual kit reagents are needed.



Description: Echelon’s β-catenin/Tcf protein-protein interaction assay is a fluorescence polarization (FP) assay designed for high throughput screening in a 384-well format for small molecule inhibition or the β-catenin:Tcf protein-protein interaction.

β-catenin is a key mediator for the Wnt pathway. The Wnt pathway is classified as a β-catenin-dependent pathway or β-catenin-independent pathway. The Wnt/β-catenin-dependent pathway is responsible for many cellular regulations such as proliferation, differentiation and cell-cell communication. Hyperactivated Wnt/β-catenin-dependent pathway triggers progression of many cancers such as colorectal cancers, liver cancer, breast cancer, etc. The transcription of the overactive Wnt/β-catenin-dependent pathway is solely dependent on the nuclear β-catenin:T-cell factor (Tcf) binding. Thus, inhibitors targeting the β-catenin/Tcf protein-protein interaction appear to be a promising therapeutic strategy for cancer. Lately, literature suggests activation of the β-catenin/Tcf signaling by the lipid growth factor, lysophosphatidic acid (LPA), may be involved in neurogenesis as well.

Echelon’s β-catenin/Tcf protein-protein interaction assay is a fluorescence polarization (FP) assay designed for high throughput screening in a 384-well format for small molecule inhibition or the β-catenin:Tcf protein-protein interaction. The β-catenin protein used in this assay is a partial protein which includes the domain that binds to the human Tcf. A selected short peptide sequence of the human Tcf with TAMRA label (Tcf-TAMRA) is used in the assay. When β-catenin binds to the Tcf-TAMRA, the TAMRA fluorophore’s rotational movement becomes slower due to the increase in molecular mass and thus the emitted light remains polarized (figure 1). Therefore, the inhibition between β-catenin and Tcf-TAMRA binding can be monitored by the change in polarization of light. PKF118-310 (Lepourcelet 2004) is included in the assay as a control inhibitor.

Storage

Upon receipt, store kit at -20°C. Allow the reagents to warm to room temperature. Centrifuge vials before opening.

References

1) Lepourcelet, M, Chen, YN, et al. Small molecule antagonists of the oncogenic Tcf/beta-catenin protein complex. Cancer Cell. 5(1), 91-102 (2004).
2) Zhang, M, Huang, Z, et al. New homogeneous high-throughput assays for inhibitors of ?-catenin/Tcf protein–protein interactions. Anal Biochem. 424(1), 57-63 (2012).>


Options/Sizes Pricing
K-5900-1kit $ 450.00
Additional Information:
Tech Data Sheet - TDS K-5900 Rev6


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assay and reagents for drug discovery in lipid signaling pathways