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.
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- No. CAS: 1586007-00-2
- Fòrmula: C37H41ClN4O9
- Peso molecular:721.20
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
Actividad biológica
Descripciòn
Cellular Effect
|
Cell Line
|
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.
Chemical Information
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No. CAS 1586007-00-2
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Peso molecular 721.20
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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)