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-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].

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

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

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 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 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.

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.

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.

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.

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

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

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.

ICG001 is a β-catenin TCF-mediated transcription inhibitor that selectively blocks β-catenin CBP interaction without interfering with β-catenin p300 interaction. It specifically binds to CREB protein with an IC50 of 3 μM.

TNIK-IN-5 is an potent TNIK inhibitor (IC50= 0.05 μM). TNIK-IN-5 potently inhibits Wnt signaling in intact cells. TNIK-IN-5 exhibits excellent in vitro anti-colorectal cancer activity.

NRX-103094 is a potent enhancer of the interaction between β-catenin and the homologous E3 ligase SCFβ-TrCP, increasing the affinity of pSer33 Ser37 β-catenin for β-TrCP with an EC50 of 62 nM and a Kd of 0.6 nM.

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

GSK-3β inhibitor 8 (GSK3β Inhibitor XVIII) is a potent and selective GSK-3β inhibitor with an IC50 value of 64 nM.GSK-3β inhibitor 8 is a thienopyrimidine derivative that negatively regulates the Wnt signaling pathway and stimulates β-cell proliferation.

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.

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.

Carboxylesterase-IN-3 is a potent inhibitor of Carboxylesterase Notum (IC50 ≤ 10 nM).Carboxylesterase-IN-3 has the potential to study cancer diseases.

Miclxin (DS37262926) is a novel MIC60 inhibitor that induces apoptosis through mitochondrial stress in mutant tumor cells via β-catenin.Miclxin is a potent inhibitor of mutant β-catenin, which is involved in the Wnt signaling pathway.Miclxin induces β-catenin-dependent apoptosis, leading to mitochondrial damage and loss of mitochondrial membrane. Miclxin has anti-tumor activity and kills tumors by targeting MIC60.