Wnt Inhibitor

PMED-1 is a β-catenin inhibitor that significantly reduces β-catenin activity in hepatoblastoma cells and various HCC cells, with an IC₅₀ value ranging from 4.87 to 32 μM. PMED-1 affects Wnt signaling by decreasing the interaction between β-catenin and CREB binding protein, thereby inhibiting cell proliferation. PMED-1 has potential applications in cancer research.

BIM-46174 is a heterotrimeric G protein complex inhibitor. BIM-46174 blocks GPCR downstream signaling by trapping Gα proteins in a nucleotide-free pocket conformation, thereby inhibiting Gαq-mediated calcium release, Gαs-mediated cAMP production, and GPCR-regulated cancer cell invasion. In vitro, BIM-46174 effectively suppresses a variety of clinically multidrug-resistant cell lines and induces tumor cell apoptosis through activation of caspase-3 and PARP cleavage. BIM-46174 also inhibits activation of the Neu1-MMP-9-GPCR signaling platform and downstream NF-κB signaling, and is widely used in the study of cancer signaling pathways and inflammation-related research, including lung cancer, pancreatic cancer, breast cancer, melanoma, and leukemia.

Pizotifen (Standard) (Pizotyline (Standard)) is the analytical standard of Pizotifen (HY-B0115). This product is intended for research and analytical applications. Pizotifen (Pizotyline) is a 5-HT₂ receptor antagonist. Pizotifen inhibits the Wnt/β-catenin-EMT signaling pathway and induces mitochondria-mediated Apoptosis. Pizotifen causes transient ERK1/2 phosphorylation and restores ATP. Pizotifen blocks Serotonin (HY-B1473A)-mediated platelet activation, inhibits Serotonin-enhanced ADP-induced platelet aggregation, and prolongs carotid artery occlusion and tail bleeding time. Pizotifen exhibits anticancer activity against gastric cancer and colon cancer. Pizotifen exerts neuroprotective effects in the striatum of R6/2 mice. Pizotifen can be used for research on gastric cancer, colon cancer, Huntington's disease, metastasis, and thromboembolic diseases.

GNF-6231 (Standard) is the analytical standard of GNF-6231 (HY-100408). This product is intended for research and analytical applications. GNF-6231 is a porcupine (IC50= 0.8 nM), Pron, and endoplasmic reticulum protein inhibitor with oral activity. GNF-6231 has anticancer activity. GNF-6231 can prevent the activation of the Wnt pathway by blocking the secretion of all Wnt ligands. GNF-6231 can be used in the study of myocardial infarction.

Sapanisertib (INK-128; MLN0128; TAK-228) Standard is the analytical standard of Sapanisertib (HY-13328). This product is intended for research and analytical applications. Sapanisertib (INK-128; MLN0128; TAK-228) is an orally active dual mTORC1/mTORC2 inhibitor. Sapanisertib directly and simultaneously inhibits mTORC1/2 activity through competitive binding with ATP, thereby comprehensively blocking downstream processes such as protein and lipid synthesis and cytoskeletal reorganization, consequently suppressing tumor cell proliferation and promoting apoptosis. Sapanisertib is applicable to research on melanoma, ovarian cancer, pulmonary fibrosis, and hematological malignancies.

WHN-88 is a Porcupine (PORCN) inhibitor. WHN-88 can eliminate the palmitoylation of Wnt ligands, preventing their secretion and subsequent Wnt/β-catenin signaling. WHN-88 can inhibit cancer cell stemness and suppress the occurrence and development of breast tumors in MMTV-Wnt1 transgenic mice.

Wnt/β-catenin-IN-4 (compound YW1159) is a potent Wnt/β-catenin inhibitor.

Specnuezhenide (Standard) is the analytical standard of Specnuezhenide. This product is intended for research and analytical applications. Specnuezhenide ((8E)-Nuezhenide) is isolated from the fruits of?Ligustrum lucidum. Specnuezhenide ((8E)-Nuezhenide) can inhibit IL-1β-induced inflammation in chondrocytes via inhibition of NF-κB and wnt/β-catenin signaling. Specnuezhenide ((8E)-Nuezhenide) exerts anti-inflammatory effects in a rat model of osteoarthritis (OA).

IWR-1 (Standard) is the analytical standard of IWR-1 (HY-12238). This product is intended for research and analytical applications. IWR-1 (IWR-1-endo) is a tankyrase inhibitor targeting Wnt/β-catenin (IC₅₀ = 180 nM). IWR-1 compromises critical steps of the canonical Wnt signaling, namely translocation of β-catenin to the nucleus and subsequent TCF/LEF activation and expression of Wnt/β-catenin downstream targets. IWR-1 promotes β-catenin phosphorylation by promoting stability of Axin-scaffolded destruction complexes. IWR-1 can be studied in research for anti-tumor purposes, and diseases such as osteosarcoma, colorectal cancer and psoriasis.

Sempervirine is an alkaloid derived from Gelsemium elegans Benth.. Sempervirine inhibits the proliferation of hepatocellular carcinoma (HCC) cells and induces apoptosis by regulating Wnt/β-catenin pathway.

Tizanidine (Standard) is the analytical standard of Tizanidine (HY-B0194). This product is intended for research and analytical applications. Tizanidine, a skeletal muscle relaxant, is an orally effective central α₂-adrenoceptor agonist (IC₅₀ = 6.9 nmol). Tizanidine primarily exerts muscle relaxation effects by inhibiting the release of excitatory amino acids (glutamate and aspartate) from the presynaptic terminals of spinal cord interneurons. Tizanidine has anti-injury activity and can inhibit gastrointestinal (GI) transport. Tizanidine can inhibit the proliferation, migration, and invasion of lung cancer cells and induce cell apoptosis by upregulating Nischarin and inhibiting the AKT and Wnt3a/β-catenin signaling pathways. Tizanidine can be used to treat spasticity caused by diseases such as multiple sclerosis (MS), stroke, and spinal cord injury (SCI).

Combretastatin A-1 (Standard) is the analytical standard of Combretastatin A-1. This product is intended for research and analytical applications. 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.

AMG-167 is an anti-cancer monoclonal antibody targeting sclerostin. AMG-167 can be studied in research for osteoporosis.

NCB-0846 (Standard) is the analytical standard of NCB-0846 (HY-100830). This product is intended for research and analytical applications. 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.

LZZ-02 (ZINC13406363) is an orally active Tankyrase 1/2 inhibitor. LZZ-02 reduces c-Myc levels and inhibits the transcriptional activity of the WNT/β-catenin pathway. LZZ-02 exhibits anticancer activity against colon cancer. LZZ-02 can be used in studies related to colorectal cancer.

MSAB (Standard) is the analytical standard of MSAB (HY-120697). This product is intended for research and analytical applications. MSAB is a potent and selective inhibitor of Wnt/β-catenin signaling. MSAB binds to β-catenin and promotes its degradation, and specifically downregulates Wnt/β-catenin target genes. MSAB exhibits potent anti-tumor effects selectively on Wnt-dependent cancer cells.

5T4_0108 (MEDI0641 antibody) is a human monoclonal antibody (mAb) targeting TPBG. 5T4_0108 can be used in breast and prostate cancer research.

IWP-12 (Standard) is the analytical standard of IWP-12 (HY-107570). This product is intended for research and analytical applications. IWP-12 is a potent inhibitor of porcupine (PORCN) and inhibits cell-autonomous Wnt signaling with an IC₅₀ of 15 nM.

Nimbolide (Standard) is the analytical standard of Nimbolide. This product is intended for research and analytical applications. 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.

Cyflumetofen (Standard) is the analytical standard of Cyflumetofen (HY-W663938). This product is intended for research and analytical applications. Cyflumetofen is a non-systemic acylacetonitrile Acaricide. Cyflumetofen interferes with the Wnt/β-catenin signaling pathway, induces Apoptosis, and reduces the level of tight junction proteins. Cyflumetofen upregulates the expression of Pink1, Parkin and Lrrk2 genes associated with the pathogenesis of Parkinson's disease in zebrafish larvae. Cyflumetofen induces developmental toxicity and oxidative stress in zebrafish larvae, damages neurons, reduces motor activity, alters brain tissue structure, and disrupts blood-brain barrier structure. Cyflumetofen exhibits acaricidal activity against spider mites. Cyflumetofen can be used in studies related to Parkinson's disease and infestations by spider mites (Tetranychus urticae, Tetranychus kanzawai, Panonychus citri).