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^[1].

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.

437.41

C₂₃H₁₅N₇O₃

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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• [1]. Deng Y, et al. Design, Synthesis, and Structure-Activity Relationship of 2-(Piperazin-1-yl)quinazolin-4(3H)-one Derivatives as Active Agents against Toxoplasma gondii. J Agric Food Chem. 2025 Mar 12;73(10):6215-6230.