β-catenin

β-catenin modulator IIa-661 is a small molecule inhibitor of the Wnt pathway with antitumour activity.

β-catenin/CBP-IN-1 is a potent and selective inhibitor of CBP/β-catenin

Wnt/β-catenin agonist 1 is an agonist of Wnt/β-catenin signalling pathway(EC50 of 0.27 μM).

β-Catenin modulator-8 (Compound Ⅸa) is a specific β-catenin modulator for use in cancer research.

TCF4/β-catenin-IN-1 (Compound 8b) is an inhibitor of TCF4/β-catenin that induces apoptosis. This compound enhances the expression of p53, caspase-3, caspase-8, caspase-9, and Bax proteins, while reducing Bcl-2 protein levels. TCF4/β-catenin-IN-1 also inhibits CYP3A4, CYP1A2, and CYP2C19, demonstrating significant cytotoxic activity in cancer cells.

Wnt/β-catenin activator 1 (Compound 5m) is an orally active activator of the Wnt/β-catenin signaling pathway. It induces cell cycle arrest in the G1 phase, inhibits early proliferation of adipocytes, and suppresses adipogenesis in 3T3-L1 cells with an IC50 of 330 nM. In a high-fat diet-fed Syrian golden hamster model, Wnt/β-catenin activator 1 exhibits anti-adipogenic and anti-dyslipidemic activities.

TFAP4/Wnt/β-catenin-IN-1 (Compound A61) is an orally active inhibitor targeting the TFAP4/Wnt/β-catenin pathway. Known for its potent anticancer properties, it effectively targets various cancer cells, including those of gastric, lung, and breast cancer, with the strongest activity observed in MGC-803 gastric cancer cells (IC50: 3.92 μM). By inhibiting the TFAP4/Wnt/β-catenin signaling pathway, it induces apoptosis and S phase cell cycle arrest. TFAP4/Wnt/β-catenin-IN-1 is applicable for gastric cancer research.

Wnt/β-catenin-IN-6 (compound B10) is a potent inhibitor of the Wnt/β-catenin signaling pathway. It effectively suppresses the activity of A549 cells, with an IC50 of 1.28 μM.

β-catenin/BCL9 PPI-IN-1 (compound B4) is an effective inhibitor of the interaction between β-catenin and B-cell lymphoma 9 proteins (β-catenin/BCL9 PPI), with an IC50 value of 2.25 μM.

Wnt/β-catenin-IN-1 (compounds 17) is an inhibitor of the Wnt/β-catenin signaling pathway. It induces apoptosis in colon cancer cells and exhibits broad-spectrum anticancer activity, making it useful for research on various solid tumors.

β-Catenin-IN-37 is a selective inhibitor of the protein-protein interaction between β-Catenin and T-cell factor (Tcf), known as β-catenin/Tcf PPI. It effectively inhibits canonical Wnt signaling and impedes the growth of colorectal cancer cells SW480 and HCT116, with IC50 values of 20 μM and 31 μM, respectively.

Wnt/β-catenin agonist 4 is an agonist of Wnt that activates Wnt/β-catenin signaling and directs signaling.

β-catenin-IN-3 is a selective and potent β-catenin inhibitor (KD: 54.96 nM) that targets a cryptic regulatory site of β-catenin and significantly reduces the viability of β-catenin-driven cancer cells.

β-Catenin-IN-4 is a β-catenin inhibitor characterized by a K_i value of 0.64 μM. This compound effectively lowers the protein expression levels of cyclin D1 and c-Myc.

β-Catenin-IN-6 is an inhibitor of the canonical Wnt/β-catenin signaling pathway, effectively impeding the proliferation of human colorectal cancer cells and demonstrating efficacy in a β-catenin/RK3E mouse model [1] [2].

β-Catenin-IN-7 (Compound 9) is an inhibitor of β-catenin that disrupts its interaction with Tcf-4, consequently impeding Wnt-dependent gene expression, and exhibits anticancer activity [1].

β-Catenin modulator-1 (IIa-650) is a valuable agent in cancer research for modulating β-Catenin [1].

β-Catenin Modulator-2 (Compound IIa-130), which is an oxazole-thiazole derivative, serves as a potent and selective modulator of β-Catenin [1].

β-Catenin modulator-3 (compound IIa-112), an oxazole and thiazole-based chemical entity, serves as a potent and selective modulator of β-Catenin [1].

β-Catenin modulator-4 (compound IIa-92), containing oxazole and thiazole moieties, functions as a potent and selective β-Catenin modulator [1].

β-Catenin Modulator-5 (Compound IIa-84), an oxazole and thiazole-based compound, serves as a potent and selective modulator of β-Catenin [1].

hCA/Wnt/β-catenin-IN-1 (Compd 15) is an inhibitor selectively targeting hCA isoforms II, IX, and XII, with K i values of 33.6, 24.1, and 6.8 nM, respectively. It also attenuates P-gp activity, disrupts the Wnt/β-catenin signaling pathway, and compromises the viability of cancer cells, specifically against the NCI/ADR-RES DOX-resistant cell line [1].

PTK7/β-catenin-IN-1 (compound 01065) is a potent inhibitor targeting PTK7/β-catenin and p53/MDM2, with IC50 values of 8.9 μM and 56.5 μM, respectively. This compound shows promise for cancer research applications [1].

Wnt/β-catenin-IN-3 (compound 17), a Wnt/β-catenin inhibitor, exhibits low micromolar GI 50 s across different cancer cell lines. It induces G2/M cell cycle arrest through the activation of the p53-p21 pathway and promotes both intrinsic and extrinsic apoptotic death in colon cancer cells [1].