Wnt/beta-catenin

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.

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.

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

XAV-939 (NVP-XAV939) is a Tankyrase (TNKS) inhibitor that inhibits TNKS1 and TNKS2 (IC50=11 4 nM). XAV-939 selectively inhibits Wnt β-catenin-mediated transcription.

Romosozumab (AMG-785) is a humanized monoclonal antibody that binds and inhibits sclerostin, increasing bone formation and decreasing bone resorption.Romosozumab is used in the study of postmenopausal osteoporosis.

Heparan sulfate is a natural product, a linear polysaccharide. Heparan sulfate occurs as a proteoglycan (HSPG) that is tightly attached to cell surface or extracellular matrix proteins.

1. Xanthatin has cytotoxic activity. 2. Xanthatin has antibacterial and antifungal activies against MRSA. 3. Xanthatin may have therapeutic potential against NSCLC. 4. Xanthatin can inhibit murine melanoma B16-F1 cell proliferation possibly associated wit

Echinacoside is a natural polyphenolic compound with various kinds of pharmacological activities, such as anti-inflammatory, antioxidative, hepatoprotective, neuroprotective, nitric oxide radical-scavenging and vasodilative ones.

(-)-Agelastatin A is a member of the pyrrole-aminoimidazole marine alkaloid (PAI) family, capable of inhibiting β-catenin, GSK-3β, and osteopontin (OPN), exhibiting antiproliferative activity against various cancers such as leukaemia and breast cancer, and possessing a certain ability to penetrate the central nervous system (CNS).

Toxoflavin (Xanthothricin) is an antagonist of the transcription factor 4 (TCF4) β-catenin complex and also inhibits KDM4A.

Salinomycin (Procoxacin), a polyether potassium ionophore antibiotic, specifically inhibits the growth of gram-positive bacteria, acts as a potent inhibitor of Wnt β-catenin signaling by blocking Wnt-induced LRP6 phosphorylation, and demonstrates selective activity against human cancer stem cells.

Gossypolone is is a proposed major metabolite of gossypol. Gossypolone reduces Notch Wnt signaling and induces apoptosis.

IWR-1 (IWR-1-endo), a Wnt pathway inhibitor, stabilizes the Axin destruction complex(EC50=0.2 uM).

ICG001 antagonizes Wnt β-catenin TCF-mediated transcription and specifically binds to element-binding protein (CREB)-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300.

Wnt-C59 (C59) is a highly effective and specific Wnt signaling antagonis with PORCN enzymatic activity.

PRI-724 is a second-generation, selective small molecule inhibitor of the β-catenin CBP interaction.

1. Isoquercetin (3-Glucosylquercetin) is a potential stimulator of bone mineralization used for prophylaxis of osteoporotic disorders. 2. Isoquercetin may be as a potential therapeutic agent against neurodegeneration in Parkinson's disease. 3. Isoquercetin is an inhibitor of Wnt β-catenin and may be as a potential novel anti-tumoral agent, such as against human pancreati,liver cancer related to opioid receptors and to the activation of the mitogen-activated protein kinase (MAPK) signalling pathway. .

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.

Laduviglusib trihydrochloride (CT99021 trihydrochloride) is a selective glycogen synthase kinase 3 (GSK-3) inhibitor with IC50s of 10 nM and 6.7 nM for GSK-3α and GSK-3β. Laduviglusib trihydrochloride inhibits human GSK-3β with a Ki of 9.8 nM. Laduviglusib trihydrochloride is an activator of Wnt β-catenin signaling. Laduviglusib trihydrochloride induces autophagy.

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.

1. Triptonide (PG 492) is effective in the treatment of autoimmune diseases and has potent antileukemic and antitumor activities. 2. Triptonide possesses anti-inflammatory activity, upregulate the expression of IL-37, and this expression was suppressed by ERK1 2 and p38 MAPK inhibitors.

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.

Bisdemethoxycurcumin (Curcumin III) is a natural demethoxy derivative of curcumin. It is a potent activator of macrophage phagocytosis, interacting with 1α, 25-dihydroxy vitamin D3 to stimulate amyloid-β clearance by macrophages (optimal stimulation at 100 nM BDMC) [1]. More stable than curcumin in physiological media, BDMC suppresses proliferation of cancer cells [2]. It down-regulates the transcriptional coactivator p300, suppressing the Wnt β-catenin pathway, and inhibits LPS induction of iNOS expression [3].

Vantictumab (OMP-18R5) is a humanized anti-FZD1 2 5 7 8 monoclonal antibody that inhibits Wnt pathway signaling and is used in research studies for the treatment of metastatic HER2-negative breast cancer and metastatic pancreatic adenocarcinoma.