Wnt Inhibitor

NCB-0846 is an orally active, selective inhibitor for Wnt, that inhibits Traf2- and Nck-interacting kinase (TNIK) with an IC₅₀ of 21 nM. NCB-0846 blocks TGF-β signaling pathway by inhibiting SMAD2/3 phosphorylation and nuclear translocation.

FH535 is an inhibitor of Wnt/β-catenin and PPAR with anti-tumor activities.

Triptonide (NSC 165677) is a natural product identified in Tripterygium wilfordii Hook F.. Triptonide is a Wnt signaling inhibitor with an IC₅₀ of appropriately 0.3 nM. Triptonide has immunosuppression, anti-inflammatory, anti-fertility, neuroprotective and anti-lymphoma effects.

ETC-159 (ETC-1922159) is a potent, orally available PORCN inhibitor. ETC-159 inhibits β-catenin reporter activity with an IC₅₀ of 2.9 nM.

xStAx-VHLL is a β-catenin PROTAC degrader that promotes ubiquitination and proteasome degradation of β-catenin. xStAx-VHLL inhibits the Wnt/β-catenin signaling pathway. xStAx-VHLL can inhibit the proliferation of colon cancer cells and has anti-tumor activity.

Vantictumab (OMP-18R5) is a fully human IgG2 monoclonal antibody. Vantictumab inhibits Wnt pathway signaling by binding to FZD1/2/5/7/8 receptors. Vantictumab can be studied against cancers through direct actions on tumor cells, including CSCs, and effects on the stroma, such as metastatic HER2-negative breast cancer and metastatic pancreatic adenocarcinoma.

IWP-4 is a Wnt inhibitor with an IC₅₀ of 25 nM. IWP-4 specifically inhibits casein kinase 1δ/ε (CK1δ/ε), with an IC₅₀ of 1.06 μM against wild-type CK1δ, 1.02 μM against the CK1δ kinase domain, and 7.07 μM against CK1ε; it shows enhanced inhibitory activity against the M82F CK1δ mutant (IC₅₀ = 0.14 μM). IWP-4 is applicable to research related to cancer, Alzheimer's disease (AD), and heart failure.

16,16-Dimethyl prostaglandin E2 (16,16-dimethyl PGE2) is an orally active vertebrate Hematopoietic stem cells (HSCs) homeostasis critical regulator. 16,16-Dimethyl prostaglandin E2 can act through EP2/EP4 and has an interaction with the Wnt pathway.

WIKI4 is a potent tankyrase inhibitor with an IC₅₀ of 26 nM for TNKS2. WIKI4 potently inhibits Wnt/β-catenin signaling and that its half-maximal response dose is 75 nM. WIKI4 mediates its effects on Wnt/β-catenin signaling by inhibiting the enzymatic activity of TNKS2. WIKI4 is cytotoxic to SCLC cells with an IC₅₀ value of 0.02 μM.

Prodigiosin (Prodigiosine) is a red pigment produced by bacteria as a bioactive secondary metabolite. Prodigiosin is a potent inhibitor of the Wnt/β-catenin pathway. Prodigiosin has antibacterial, antifungal, antiprotozoal, antimalarial, immunosuppressive, and anticancer properties.

Cardamonin can be found from cardamom, and can target various signaling molecules, transcriptional factors, cytokines and enzymes. Cardamonin can inhibit mTOR, NF-κB, Akt, STAT3, Wnt/β-catenin and COX-2. Cardamonin shows anticancer, anti-inflammatory, antimicrobial and antidiabetic activities.

Nimbolide is a triterpene compound that can be isolated from neem (Azadirachta indica), possesses anticancer and antiproliferative activity. Nimbolide induces tumor cell apoptosis by inhibiting NF-κB and CDK4/CDK6 kinase. Nimbolide suppresses the Wnt, PI3K-Akt, MAPK and JAK-STAT signaling pathways.

EMT inhibitor-1 is an inhibitor of of Hippo, TGF-β, and Wnt signaling pathways with antitumor activities.

PNU-74654 is an inhibitor of Wnt/β-catenin pathway with an IC₅₀ of 129.8 μM in NCI-H295 cell.

DIF-3 is an orally active anticancer agent. DIF-3 reduces the expression levels of cyclin D1 and c-Myc by facilitating their degradation via activation of GSK-3β. DIF-3 inhibits Wnt/β-catenin signaling pathway-related proteins in cells. DIF-3 induces reactive oxygen species (ROS) and autophagy. DIF suppresses the growth of Trypanosoma. cruzi in HT1080 cells. DIF-3 exerts antitumor effects both in vitro and in vivo.

ZY-444 is an anti-cancer agent, targeting pyruvate carboxylase (PC). ZY-444 suppresses the Wnt/β-catenin/Snail signaling pathway by blocking nuclear translocation of β-catenin. ZY-444 selectively inhibits proliferation, migration, and invasion and induces apoptosis in cancer cells. ZY-444 exhibits potent anti-tumor in cancer mouse models. ZY-444 can be used for the study of breast cancer, lung cancer (NSCLC), prostate cancer and iodine-refractory thyroid cancer.

xStAx-VHLL TFA is a β-catenin PROTAC degrader that promotes ubiquitination and proteasome degradation of β-catenin. xStAx-VHLL TFA inhibits the Wnt/β-catenin signaling pathway. xStAx-VHLL TFA can inhibit the proliferation of colon cancer cells and has anti-tumor activity.

CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with an IC₅₀ of 5 nM in 7dF3 cells. CCT251545 is a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.

KYA1797K is a potent and selective Wnt/β-catenin inhibitor with an IC₅₀ of 0.75 µM.

Raddeanin A is an oleanane-type triterpenoid saponin with oral activity. Raddeanin A inhibits SRC, mTOR, JNK, VEGFR2, NLRP3 inflammasome, Wnt/β-catenin, Wee1, PI3K/AKT signaling pathway, MAPK/ERK signaling pathway, AR-FL, AR-Vs, and downregulates the expression of p-PI3K and p-AKT. Raddeanin A inhibits osteoclast formation, bone resorption, osteolysis, cancer cell invasion, migration, proliferation, angiogenesis and epithelial-mesenchymal transition, while induces apoptosis, cell cycle arrest, ROS production, immunogenic cell death and dendritic cell maturation. Raddeanin A improves blood-retinal barrier function, alleviates inflammation, regulates the tumor microenvironment, and enhances the activity of anti-PD-1 antibody. Raddeanin A is applicable to the research of breast cancer-associated osteolysis, human osteosarcoma, colorectal cancer, glioblastoma, Alzheimer's disease, cholangiocarcinoma, melanoma, non-small cell lung cancer, castration-resistant prostate cancer and multiple myeloma.