Wnt–β-catenin

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

Wnt β-catenin-IN-5 (Compound 4) functions as an inhibitor of the Wnt β-catenin signaling pathway. This compound effectively eradicates colorectal cancer stem cells and inhibits tumor growth by suppressing the Wnt signaling pathway. Additionally, Wnt β-catenin-IN-5 promotes the degradation of KDM3A and KDM3B.

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.

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.

Wnt/β-catenin agonist 2 activates Wnt/β-catenin signaling and is an effective Wnt agonist. Wnt/β-catenin agonist 2 can be used in the study of diseases related to signal transduction and is closely related to cancer invasion and metastasis.

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

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].

Wnt β-catenin-IN-2 (Compound 3235-0367) serves as an inhibitor of the Wnt β-catenin signaling pathway, exhibiting IC50 and KD values of 7.1 and 2.5 μM, respectively. It is applicable in cancer research [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].

Wnt/β-catenin agonist 3 is a Wnt/beta-catenin agonist.

CHIR-99021 (CT99021) is an activator of the Wnt/β-catenin signaling pathway and a GSK-3α/β inhibitor (IC50=10/6.7 nM) with selective and oral activity.CHIR-99021 induces cellular autophagy, which enhances self-renewal in mouse and human embryonic stem cells.

IWP-2 is a Wnt pathway inhibitor (IC50=27 nM) and an ATP-competitive CK1δ inhibitor (IC50=40 nM for M82FCK1δ). IWP-2 inhibits self-renewal of embryonic stem cells and has been used in stem cell and organoid research.

BML-284 (Wnt agonist 1) is a potent, selective and , cell-permeable Wnt signaling activator.

1. Ginkgetin has anti-influenza virus and anti-fungal activities. 2. Ginkgetin has anti-inflammatory activity, can down-regulates COX-2 induction in vivo against skin inflammatory responses. 3. Ginkgetin is a good STAT3 inhibitor and may be a useful lead

Adavivint (SM04690) is a selective inhibitor of the typical Wnt signaling pathway. In SW480 cells, EC50=19.5 nM was measured using high-throughput TCF/LEF reporter gene experiments.

SKL2001, an agonist of the Wnt/β-catenin pathway, can disrupt the Axin/β-catenin interaction.

MSAB is a selective inhibitor of Wnt/β-catenin signaling. MSAB binds to β-catenin, promoting its degradation, and specifically downregulates Wnt/β-catenin target genes.

HLY78 (4-Ethyl-5-methyl-5,6-dihydro-[1,3]dioxolo[4,5-j]phenanthridine) targets the DIX domain of Axin, is an activator of the Wnt/β-catenin signaling pathway and can enhance Axin-LRP6 binding to promote Wnt signaling.

Wnt pathway activator 2, with an IC50 of 13 nM, is a potent Wnt activator.

DK419 is an orally active inhibitor of Wnt/β-catenin signaling, with an IC50 of 0.19 μM. DK419 decreases protein lelvels of Axin2, β-catenin, c-Myc, Cyclin D1 and Survivin.It also induces production of pAMPK.

CCT 031374 hydrobromide is a TCF/β-catenin inhibitor with antitumor activities.

FzM1, a negative allosteric modulator (NAM) of the Frizzled receptor FZD4, diminishes WNT5A-dependent WNT responsive element (WRE) activity (log EC50inh=−6.2) by binding to an allosteric site on intracellular loop 3 (ICL3) of FZD4. This interaction changes the receptor's conformation and inhibits the WNT/β-catenin signaling pathway.