UU-T03
UU-T03 is a β-catenin/Tcf protein-protein interaction inhibitor and an inhibitor of Wnt signaling activation. UU-T03 downregulates the expression of AXIN2, LGR5, cyclin D1, and c-myc. UU-T03 inhibits the growth of colorectal cancer cells. UU-T03 can be used for research on colorectal cancer.
For research use only. We do not sell to patients.
- CAS No.: 1586007-00-2
- Formula: C37H41ClN4O9
- Molecular Weight:721.20
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SW480 | IC50 |
28.73 μM
|
Inhibition of Wnt-responsive luciferase activity in human SW480 colorectal cancer cells transfected with TOPFlash reporter.
Inhibition of Wnt-responsive luciferase activity in human SW480 colorectal cancer cells transfected with TOPFlash reporter.
|
24191653 |
| HEK293 | IC50 |
37.57 μM
|
Inhibition of Wnt-responsive luciferase activity in Wnt-activated human HEK293 cells co-transfected with β-catenin and TOPFlash reporter.
Inhibition of Wnt-responsive luciferase activity in Wnt-activated human HEK293 cells co-transfected with β-catenin and TOPFlash reporter.
|
24191653 |
| SW480 | IC50 |
10.77 μM
|
Antiproliferative activity against human SW480 colorectal cancer cells assessed as growth inhibition by MTs assay.
Antiproliferative activity against human SW480 colorectal cancer cells assessed as growth inhibition by MTs assay.
|
24191653 |
| HT-29 | IC50 |
11.01 μM
|
Antiproliferative activity against human HT29 colorectal cancer cells assessed as growth inhibition by MTs assay.
Antiproliferative activity against human HT29 colorectal cancer cells assessed as growth inhibition by MTs assay.
|
24191653 |
| HCT-116 | IC50 |
28.83 μM
|
Antiproliferative activity against human HCT116 colorectal cancer cells assessed as growth inhibition by MTs assay.
Antiproliferative activity against human HCT116 colorectal cancer cells assessed as growth inhibition by MTs assay.
|
24191653 |
| HEK293 | IC50 |
84.02 μM
|
Cytotoxicity against normal human HEK293 cells assessed as cell viability reduction by MTs assay.
Cytotoxicity against normal human HEK293 cells assessed as cell viability reduction by MTs assay.
|
24191653 |
In Vitro
UU-T03 (Compound 21) inhibits Wnt-responsive luciferase activity in SW480 and Wnt-activated HEK293 cells with IC50 values of 28.73 µM and 37.57 µM, respectively, without affecting FOPFlash activity[1].
UU-T03 downregulates AXIN2, LGR5, cyclin D1, and c-myc mRNA in SW480 cells in a dose-dependent manner[1].
UU-T03 (7.5-60 µM) reduced cyclin D1 and c-myc protein levels in SW480 cells without affecting β-catenin protein[1].
UU-T03 (0-60 µM) selectively disrupts β-catenin/Tcf interactions in HCT116 cells in a dose-dependent manner, without affecting β-catenin/cadherin and β-catenin/APC interactions[1].
UU-T03 inhibited the growth of SW480, HT29, and HCT116 colorectal cancer cells with IC50 values of 10.77, 11.01, and 28.83 µM, respectively, and exhibited an IC50 of 84.02 µM in normal HEK293 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 1586007-00-2
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Molecular Weight 721.20
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Formula C37H41ClN4O9
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SMILES
C(C(N[C@@H](CC1=CC2=C(C=C1)C=CC=C2)C(N[C@H](C(N[C@@H](CCC(OCC)=O)C(OC)=O)=O)CC(OCC)=O)=O)=O)C=3NC=4C(C3)=CC(Cl)=CC4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Pull-down
The pull-down assay is an in vitro technique used to detect physical interactions between two or more proteins and an invaluable tool for confirming a predicted protein-protein interaction or identifying novel interacting partners. This method typically involves the use of affinity purification with various wash and elution steps.
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Immunoprecipitation
Immunoprecipitation (IP) is an experimental method that uses the principle of antibody specific binding to purify and enrich target proteins.
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Protocol for Bimolecular Fluorescence Complementation (BiFC) Assay
Bimolecular fluorescence complementation detects protein-protein proximity in living or fixed cells by fusing two candidate interaction partners to nonfluorescent N- and C-terminal fragments of a fluorescent protein; when the partners interact or remain close enough, the fluorescent fragments complement, mature, and generate a fluorescent signal at the site of the protein complex. The BiFC readout is fluorescence intensity and subcellular localization of the reconstituted fluorophore, which reflects formation or stabilization of a protein complex rather than direct biochemical binding kinetics; BiFC is therefore useful for mapping where interactions occur in cancer cells, neurons, macrophages, organoid-derived cells, or drug-screening systems, but results should be validated by independent assays such as co-IP or Western blot. BiFC signal formation is delayed by fluorophore maturation and can stabilize otherwise transient complexes, so it is not a real-time reversible interaction assay
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Co-Immunoprecipitation
Co-immunoprecipitation technology can verify protein interaction based on the specific immune reaction between antibodies and antigens.
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Protocol for Yeast Two-Hybrid (Y2H) Assay
The yeast two-hybrid assay detects binary protein-protein interactions by separating a transcription factor into a DNA-binding domain fused to a "bait" protein and a transcriptional activation domain fused to a "prey" protein; if bait and prey interact in yeast, the transcription factor is reconstituted and activates reporter genes such as HIS3, ADE2, lacZ, MEL1, or other selectable/readable reporters. The readout is yeast growth on selective medium and/or reporter activity, which reflects proximity-dependent transcriptional activation in the yeast nucleus rather than direct biochemical binding in the original mammalian, tumor, neuronal, macrophage, or organoid context. Because yeast two-hybrid can generate false positives and false negatives, interaction claims should be validated using independent assays such as co-immunoprecipitation, Western blot, immunofluorescence colocalization, BiFC, pull-down, or mammalian two-hybrid assays.
Purity & Documentation
References
[1]. Huang Z, et al. Targeting the Tcf4 G13ANDE17 binding site to selectively disrupt β-catenin/T-cell factor protein-protein interactions. ACS chemical biology. 2014 Jan 17;9(1):193-201. [Content Brief]
[2]. Pećina-Šlaus N, et al. Wnt Signaling Inhibitors and Their Promising Role in Tumor Treatment. International journal of molecular sciences. 2023 Apr 04;24(7):6733. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)