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.

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.

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.

KY-02327, a metabolically stabilized analog of KY-02061, serves as a potent inhibitor of the Dishevelled (Dvl)-CXXC5 interaction. This compound activates the Wnt β-catenin pathway, thereby promoting osteoblast differentiation.

Mirodenafil is a PDE-5 inhibitor developed for the treatment of erectile dysfunction.

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.

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

Mirodenafil dihydrochloride is a PDE-5 inhibitor developed for the treatment of erectile dysfunction.

(-)-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).

xStAx-VHLL TFA is a β-catenin degrader formed by coupling xStAx to VHL ligand, has anti-cancer activity, inhibits Wnt signaling, and can be used in the study of cancer.

CHIR-99021 HCl (Laduviglusib HCl) is a highly potent and selective inhibitor of GSK-3α/β, with IC50 values of 10 nM and 6.7 nM respectively. It demonstrates remarkable selectivity for GSK-3, with over 500-fold selectivity over CDC2, ERK2, and other protein kinases. Additionally, CHIR-99021 HCl serves as a robust activator of the Wnt/β-catenin signaling pathway. Moreover, it exhibits the ability to enhance self-renewal in both mouse and human embryonic stem cells. Furthermore, CHIR-99021 HCl induces autophagy [1] [2] [3].

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

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.

1, 2, 3, 4, 6-Pentagalloylglucose (Penta-O-galloyl-β-D-glucose) and gallic acid from Pistacia lentiscus have antimutagenic and antioxidant activities. 2. 1, 2, 3, 4, 6-Penta-O-galloyl-beta-D-glucose (PGG) possesses potent anti-proliferative and anti-invasive effects, it also has inhibition of inducible nitric oxide synthase and cyclooxygenase-2 activity. 3. PGG may serve as a model for the development of new types of anti-diabetic and anti-metabolic syndrome therapeutics. 4. 1, 2, 3, 4, 6-Penta- O -galloyl-β- d -glucose has vasodilatory and anti-inflammatory effects, it dilates vascular smooth muscle and suppresses the vascular inflammatory process via endothelium-dependent nitric oxide (NO)/cGMP signaling. 5. 1, 2, 3, 4, 6-Penta-O-galloyl-beta-D-glucose can decrease the level of extracellular hepatitis B virus (HBV) (IC5, 1. microg/ml) in a dose-dependent manner, it also can reduce the HBsAg level by 25% at a concentration of 4 microg/ml; the gallate structure of PGG may play a critical role in the inhibition of anti-HBV activity, suggests that PGG could be a candidate for developing an anti-HBV agent. 6. 1, 2, 3, 4, 6-Penta-O-galloyl-β-D-glucose has anti-parasitic activity, displays an EC5 value of 67 μM, at least 6.6-fold more effective than the standard drug benznidazole against trypomastigote forms of T. cruzi.

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

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

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

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. .

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.

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

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.