Wnt Inhibitor

YB-0158 (Wnt pathway inhibitor 2) is a reverse-turn peptidomimetic and a potent colorectal cancer stem cell (CSC) targeting agent. YB-0158 disrupts Sam68-Src interactions and induces apoptosis in CRC cells. Anti-cancer activities.

Fluc-IN-1 (Compound 3) is an inhibitor for firefly luciferase with an IC₅₀ of 25 nM. Fluc-IN-1 inhibits WNT/β-catenin signaling pathway with an IC₅₀ of 33 nM (measuring by TOPFlash assay).

NKP608 is a non-peptidic derivative of 4-aminopiperidine, a highly selective, orally active, neurokinin-1 (NK₁) receptor antagonist with IC₅₀ of 2.6 nM. NKP608 is active both in vitro and in vivo, showing extremely low affinity for NK₂, NK₃ receptors. NKP608 exerts its effects by blocking the NK₁ receptor, regulate cell proliferation and apoptosis, affect neurotransmitter functions and gastric mucosal repair mechanisms, and suppress the Wnt/β-catenin pathway in antitumor research. NKP608 is applicable to research related to various diseases, including cough, anxiety disorders, depression, gastric mucosal injury, and colorectal cancer.

SRI 37892 is a small molecule compound inhibitor of Frizzled protein 7 (Fzd7) with inhibitory activity against cancer cell proliferation (IC₅₀=2μM). SRI 37892 significantly blocks Wnt/Fzd7 signaling. SRI 3789 can be used in the research of developing cancer therapeutic agents .

F7H is a Frizzled receptor FZD7 antagonist (IC₅₀: 1.25 μM). Frizzled receptors (FZDs) influence Wnt signaling, mediating embryonic development and tissue homeostasis. F7H is a potent ligand for the FZD7 transmembrane domain (TMD).

WNT7A-IN-1 sodium (1365-0109), a WNT7A inhibitor, disrupts the protein-protein interaction between WNT7A and its receptor FZD5, resulting in the upregulation of MHC-I expression. WNT7A-IN-1 sodium significantly increases the expression of MHC-I and p-p65,while concurrently reducing the expression of active β-catenin. WNT7A-IN-1 sodium (compound F) is also a photographic sensitizer in the green spectral region.

Monensin (Monensin A), an orally active antibiotic, is an ionophore that mediates Na⁺/H⁺ exchange. Monensin is a potent Wnt signaling inhibitor. Monensin causes a marked enlargement of the multivesicular bodies (MVBs) and regulates exosome secretion. Monensin can be used for bacterial, fungal, and parasitic infections research, and shows anticancer effects.

Pizotifen malate (Pizotyline malate) is a 5-HT₂ receptor antagonist. Pizotifen malate inhibits the Wnt/β-catenin-EMT signaling pathway and induces mitochondria-mediated Apoptosis. Pizotifen malate causes transient ERK1/2 phosphorylation and restores ATP. Pizotifen malate blocks Serotonin (HY-B1473A)-mediated platelet activation, inhibits Serotonin-enhanced ADP-induced platelet aggregation, and prolongs carotid artery occlusion and tail bleeding time. Pizotifen malate exhibits anticancer activity against gastric cancer and colon cancer. Pizotifen malate exerts neuroprotective effects in the striatum of R6/2 mice. Pizotifen malate can be used for research on gastric cancer, colon cancer, Huntington's disease, metastasis, and thromboembolic diseases.

Combretastatin A-1 is a microtubule polymerization inhibitor that binds to the colchicine-binding site of tubulin. Combretastatin A-1 inhibits the Wnt/β-catenin pathway through tubulin depolymerization mediated AKT deactivation. Combretastatin A-1 exhibits anti-tumor and anti-vascular effects.

Wilforine is an orally active JAK-STAT pathway inhibitor with immunomodulatory effects and the ability to inhibit osteoclast fusion. Wilforine disrupts lipid raft integrity, reprograms cholesterol and glycosphingolipid metabolic pathways, regulates NF-κB and the complement system, and modulates the expression of various interleukins. Wilforine also inhibits the Wnt11/β-catenin signaling pathway and suppresses the proliferation of fibroblast-like synoviocytes. Wilforine can serve as a quality and pharmacokinetic marker for Tripterygium glycoside tablets, and can be applied to research on related diseases such as rheumatoid arthritis, inflammatory osteolysis, and SAPHO syndrome.

DJ-1-IN-1 (compound 797780-71-3) is a DJ-1 inhibitor. DJ-1-IN-1 exhibits antiproliferative activity in ACHN cells with an IC50 value of 12.18 μM and can inhibit the Wnt signaling pathway. DJ-1-IN-1 can be used in cancer research.

Coronaridine, an iboga type alkaloid, inhibits the wnt signaling pathway by decreasing β-catenin expression.

NLS-StAx-h TFA is a selective, cell permeable, stapled peptide Wnt signaling inhibitor with an IC₅₀ of 1.4 μM. NLS-StAx-h TFA efficiently inhibits β-catenin-transcription factor interactions. NLS-StAx-h TFA shows anti-proliferation of cancer cells.

TNIK-IN-8 (Compound 35b) is a potent, orally active TNKI inhibitor with a IC₅₀ value of 6 nM. TNIK-IN-8 has antitumor activity.

Nodosin is an orally active diterpenoid compound that can be isolated from Isodon serra. Nodosin can inhibit the proliferation and induce cell cycle arrest and apoptosis of tumor cells. Nodosin can also inhibit oxidative stress, inflammatory responses, and ferroptosis. Nodosin has anti-inflammatory and anti-tumor activities.

Wnt-C59 (C59) GMP is a GMP grade Wnt-C59 (HY-15659). GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Wnt-C59 (C59) is a highly potent and oral porcupine (PORCN) inhibitor with an IC₅₀ of 74 pM.

CKG012 is an inhibitor for Wnt/βcatenin signaling pathway. CGK012 inhibits release of HMGB1 and transcription of β-catenin, exhibits attenuating activities against cecal ligation and puncture (CLP)-induced sepsis and multiple myeloma cancer.

Gomisin M2 ((+)-Gomisin M2) is a lignan isolated from the fruits of Schisandra chinensis with oral availability. Gomisin M2 inhibits STAT1 phosphorylation as well as NF-κB p65 phosphorylation and nuclear translocation. Gomisin M2 reduces inflammatory cell infiltration, cytokine and chemokine expression, and serum IgE and IgG_2a levels. Gomisin M2 inhibits MAPK phosphorylation, IκBα degradation, and NF-κB nuclear translocation in keratinocytes. Gomisin M2 induces apoptosis, mitochondrial membrane potential disruption, and cytochrome c release, and inhibits DNA synthesis and mammosphere formation through downregulation of Wnt/β-catenin. Gomisin M2 can be used for research on atopic dermatitis, psoriasis, breast cancer, liver injury, and multidrug-resistant mammary adenocarcinoma.

PTK7/β-catenin-IN-6 (Compound 03653) is an inhibitor for PTK7/β-catenin interaction, which inhibits the Wnt signaling pathway, and exhibits an anticancer activity against colorectal cancer (CRC).

FIDAS-3 is a stilbene derivative and is a potent Wnt inhibitor with an IC₅₀ of 4.9 μM for methionine S-adenosyltransferase 2A (MAT2A). FIDAS-3 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-3 has anticancer activities.