Wnt Inhibitor

CWP232228, a highly potent selective Wnt/β-catenin signaling inhibitor, antagonizes binding of β-catenin to T-cell factor (TCF) in the nucleus. CWP232228 suppresses tumor formation and metastasis without toxicity through the inhibition of the growth of breast and liver cancer stem cells (CSCs).

SGC-AAK1-1, a chemical probe, is a potent and selective AAK1 (AP2 associated kinase 1) inhibitor with an IC₅₀ of 270 nM and a K_i of 9 nM. SGC-AAK1-1 also potently inhibits BMP2K. SGC-AAK1-1 is used to study Wnt pathway related to AAK1.

2-Hydroxyanthraquinone is a product generated by the photochemical oxidation of Anthracene (ANT) (HY-Y0299). 2-Hydroxyanthraquinone induces ferroptosis in cardiomyocytes by depleting GSH and inhibiting GPX4, leading to cardiac developmental malformations. 2-Hydroxyanthraquinone causes damage to the cerebrovascular system and blood-brain barrier in zebrafish by downregulating the Wnt/β-catenin signaling pathway, as well as inducing inflammation and neuronal apoptosis. 2-Hydroxyanthraquinone can be used in studies related to cerebrovascular diseases and cardiotoxicity.

Ipivivint (Compound 38) is an orally active and potent CDC-like kinase (CLK) inhibitor with EC₅₀ of 1 nM and 7 nM for CLK2 (human) and CLK3 (human), respectively. Ipivivint also inhibits the Wnt pathway (EC50=13 nM) and tyrosine phosphorylation-regulated kinase 1A (human) (EC₅₀=5 nM).

FzM1 is a negative allosteric modulator (NAM) of Frizzled receptor FZD4. FzM1 reduces WNT5A-dependent WNT responsive element (WRE) activity (log EC_50inh=?6.2). FzM1 binds to an allosteric binding site located in intracellular loop 3 (ICL3) of FZD4 and alters the conformation of the receptor, ultimately inhibiting the WNT/β-catenin cascade.

Miclxin (DS37262926) is a potent inhibitor of mutant β-catenin, involving in Wnt signaling pathway. Miclxin induces β-catenin-dependent apoptosis, leads to severe mitochondrial damage with the loss of mitochondrial membrane. Miclxin kills tumor via targeting to MIC60, a major components of the mitochondrial contact site and cristae organizing system (MICOS) complex.

NSC668036 is a Dishevelled (Dvl) PDZ domain inhibitor with a K_d of 237 μM. NSC668036 blocks Wnt signaling by interrupting the Frizzled-Dvl interaction.

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

Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling. Longdaysin inhibits CK1α, CK1δ, CDK7, and ERK2 with IC₅₀s of  5.6 µM, 8.8 µM, 29 µM, and 52 µM, respectively.

Pamidronate disodium pentahydrate, the second-generation nitrogen-containing bisphosphonate, is an inhibitor of bone loss. Pamidronate disodium pentahydrate significantly inhibits subchondral bone loss in early osteoarthritis by upregulating the expression of osteoprotegerin in cartilage and subchondral bone, and inhibiting the expression of RANKL and MMP-9 in both tissues, as well as TLR-4 in cartilage, thereby alleviating cartilage degeneration. Additionally, Pamidronate disodium pentahydrate can inhibit the signaling of Wnt and β-catenin, and is applicable for research on osteoporosis and osteosarcoma.

PROTAC KDM3 degrader-1 is a KDM3A/KDM3B PROTAC degrader with DC₅₀ values of 13.73 nM and 172.6 nM in SW480 cells, respectively. PROTAC KDM3 degrader-1 induces cereblon-dependent proteasomal degradation of KDM3A and KDM3B. PROTAC KDM3 degrader-1 inhibits the oncogenic Wnt/β-catenin signaling pathway. PROTAC KDM3 degrader-1 eliminates colorectal cancer stem cells, suppresses their self-renewal, and blocks colony formation of colorectal cancer cells. PROTAC KDM3 degrader-1 inhibits tumor growth in a colorectal cancer xenograft mouse model. PROTAC KDM3 degrader-1 can be used for the research of colorectal cancer.

3289-8625 is an inhibitor of the PDZ domain of Dishevelled (Dvl) protein (K_d=10.6 μM) and has an inhibitory effect on Wnt signaling. In addition, 3289-8625 can slow the growth of prostate cancer PC-3 cells (IC₅₀=12.5 μM). 3289-8625 can be used in the study of embryonic development and cancer.

2,5-Dimethylcelecoxib is an analogue of celecoxib (HY-14398) with anticancer activity but without COX-2 inhibitory activity. 2,5-Dimethylcelecoxib exerts its anti-cancer cell proliferation effect by inhibiting the core mechanism of the Wnt/β-catenin signaling pathway. 2,5-Dimethylcelecoxib also inhibits T-cell factor-dependent transcriptional activity and inhibits expression of the Wnt/β-catenin target gene products cyclin D1 and survivin.

KY02111 is a canonical WNT signaling (β-catenin) inhibitor which promotes differentiation of hPSCs to cardiomyocytes. KY02111 can be used for the research of human cardiomyocyte regeneration.

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).

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).

UU-T02 is a novel potent, selective small-molecule inhibitor of β-Catenin/T-cell factor protein-protein interaction (β-catenin/Tcf PPI) with a K_i of 1.36 μM. UU-T02 inhibits canonical Wnt signaling and the growth of colorectal cancer cells.

Wnt pathway inhibitor 3 is a potent wnt inhibitor with an IC₅₀ value of 45 nM. Wnt pathway inhibitor 3 shows antiproliferative activity.

WNTinib (APS-8-100-2) is a multi-kinase inhibitor that selectively antagonizes β-catenin (CTNNB1) mutated hepatocellular carcinoma (HCC). WNTinib downregulates oncogenicWntsignaling by inhibiting KIT/MAPK and downstream EZH2 activation.

Murrayafoline A is a carbazole alkaloid that can be extracted from Murraya tetramera. Murrayafoline A directly targets Specificity protein 1 (Sp1), thereby inhibiting NF-κB and MAPK signaling pathways. Murrayafoline a induces a G0/G1-phase arrest in platelet-derived growth factor (PDGF)-stimulated vascular smooth muscle cells. Murrayafoline A attenuates the Wnt/β-catenin pathway by promoting the degradation of intracellular β-catenin proteins. Murrayafoline A enhances the contraction of rat ventricular myocytes and L-type calcium current by activating protein kinase C. Murrayafoline A inhibits LPS (HY-D1056)-induced neuroinflammation in vivo. Murrayafoline A can be used for the study of inflammation, vascular complications and colon cancer.