TCF4/β-catenin-IN-1
TCF4/β-catenin-IN-1 (Compound 8b) is an inhibitor of TCF4/β-catenin, and induces apoptosis. TCF4/β-catenin-IN-1 up-regulates p53, caspase-3, caspase-8, caspase-9 levels and Bax protein expression as well as down-regulates Bcl-2 protein expression. TCF4/β-catenin-IN-1 can inhibit CYP3A4, CYP1A2, CYP2C19, and shows promising cytotoxic activity in cancer cells.
For research use only. We do not sell to patients.
- Formula: C23H15N7O3
- Molecular Weight:437.41
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
TCF4/β-catenin-IN-1 (0.4-100 μM, 24 h) exhibits cytotoxic activity against the HCT-116, A549 and HepG2 cancer cell lines, with IC50 values of 8.52 μM, 5.87 μM and 3.12 μM, respectively[1].
TCF4/β-catenin-IN-1 (8.52 μM, 24 h) can significantly increases p53 and pro-apoptotic Bax expression levels, and down regulates the anti-apoptotic Bcl-2 expression levels in HCT-116 cell line[1].
TCF4/β-catenin-IN-1 (5-20 μM) suppressesβ-catenin and TCF-4 expression in HCT-116 cells in a dose-dependent manner[1].
TCF4/β-catenin-IN-1 (8.52 μM) can significantly increase caspase-3, caspase-8 and caspase-9 expression levels in HCT-116 cell line[1].
TCF4/β-catenin-IN-1 can inhibit CYP3A4, CYP1A2, CYP2C19[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116, A549, HepG2
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Concentration:0.4-100 μM
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Incubation Time:24 h
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Result:Exhibited cytotoxic activity against the HCT-116, A549 and HepG2 cancer cell lines, where the IC50 values were 8.52 μM, 5.87 μM and 3.12 μM, respectively.
Chemical Information
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Molecular Weight 437.41
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Formula C23H15N7O3
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SMILES
N#CC1=C(C2=CC=C(OC)C(OC)=C2)N=C3NN=C4NC5=C(C=CC=C5)C4=C(C#N)N3C1=O
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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.
Purity & Documentation
References
[1]. Mourad MAE, et al. Novel inhibitors of oncogenic Wnt/TCF-4/β-catenin signaling pathway: Design, synthesis, molecular docking studies and apoptosis inducing activity of pyrimidothiazino-, dihydropyrimidotriazepino- and 1,3,4-thiadiazolopyrimido-indole hybrids. Bioorg Chem. 2025 Feb 26;157:108285. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TCF4/β-catenin-IN-1 Related Classifications
HY-172393 Related Classifications
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