Wnt Inhibitor

Anticancer agent 291 (Compound 2406) is an anti-cancer agent. Anticancer agent 291 interferes with the integrity of the β-tubulin cytoskeleton and inhibits the Wnt/β-catenin signal transduction. Anticancer agent 291 significantly inhibits the invasion, migration and colony formation of tumor cells. Anticancer agent 291 induces the cell cycle of EC-9706 and HT-29 cells to arrest at the G2/M phase and inhibits cell proliferation. Anticancer agent 291 can be used for the study of gastrointestinal cancer.

SEN461 is a potent and orally active Wnt pathway inhibitor. SEN461 shows effective anti-tumor activity and can be used for GBM research.

Apoptosis inducer 22 (QR-5) is an apoptosis inducer with IC₅₀ values ​​of 63.1 and 46.5 μM for colon cancer cell lines SW480 and HT29, respectively. Apoptosis inducer 22 induces apoptosis by inhibiting the Wnt/β-catenin axis in colon cancer cells. Apoptosis inducer 22 can be used in anti-colon cancer research.

Butrin is a compound found in Butea monosperma flowers. Butrin reduces expression of SIRT1, AURKB, cyclin D1, pAKT, GSK-3β, β-catenin, and TGF-3β expression, enhances apoptosis and ROS production in cancer cells. Butrin downregulates Wnt and NF-κB signaling, mitigates oxidative stress, reduces proinflammatory cytokine (TNF-α, IL-6 and IL-8) production and suppresses neuroinflammation. Butrin inhibits IKK enzyme activity. Butrin can be used for the researches of colorectal cancer, Alzheimer’s disease, and rheumatoid arthritis.

21H7 is a selective inhibitor of the Wnt/b-catenin pathway. 21H7 markedly inhibits the growth of HFs. 21H7 potently decreases growth of breast and colon cancer cells.

Pamidronic acid sodium, the second-generation nitrogen-containing bisphosphonate, is an inhibitor of bone loss. Pamidronic acid sodium 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, Pamidronic acid sodium can inhibit the signaling of Wnt and β-catenin, and is applicable for research on osteoporosis and osteosarcoma.

β-catenin-IN-7 (Compound 9) is a β-catenin inhibitor. β-catenin-IN-7 inhibits the interaction between β-catenin and Tcf-4, and inhibits Wnt-dependent target gene expression. β-catenin-IN-7 has anti-cancer activity.

Viridicatol (Standard) is the analytical standard of Viridicatol (HY-116474). This product is intended for research and analytical applications. Viridicatol is a quinolone alkaloid with anti-inflammatory, antibacterial, antifungal, osteogenic and chondrogenic activities. Viridicatol reduces the phosphorylation levels of ERK, JNK, p38 and STAT6; inhibits MMP-2, MMP-9, NF-κB signaling pathway and PTP1B; downregulates genes related to mast cell activation; and binds to SHN3 to activate the Wnt/SHN3 signaling pathway. Viridicatol inhibits the expression of pro-inflammatory mediators and cytokines, and promotes osteogenic/chondrogenic differentiation. Viridicatol can be used in studies related to fibrosarcoma, allergy, bacterial infection, fungal infection and osteoporosis.

Combretastatin A-1 phosphate (OXi-4503) tetrasodium, a proagent of Combretastatin A-1, is a microtubule polymerization inhibitor that binds to the colchicine-binding site of tubulin. Combretastatin A-1 phosphate tetrasodium inhibits the Wnt/β-catenin pathway through tubulin depolymerization mediated AKT deactivation. Combretastatin A-1 phosphate tetrasodium exhibits anti-tumor and anti-vascular effects.

RR-171 is an amino acid polypeptide and an inhibitor of the Wnt signaling pathway. RR-171 reduces the expression levels of Wnt-1, GSK3β and β-catenin. RR-171 induces apoptosis (Apoptosis) in pancreatic cancer cells, which is characterized by an increased Bax/Bcl-2 ratio, activation of Caspase-3/7/9, and increased Cleaved-PARP; this pro-apoptotic effect can be partially reversed by Z-VAD-FMK (HY-16658B). RR-171 also induces pyroptosis (Pyroptosis) in pancreatic cancer cells, which is manifested by activation of the NLRP-3 inflammasome, activation of Caspase-1, cleavage of GSDMD, upregulation of IL-1β and IL-18, and increased LDH release; this pro-pyroptotic effect can be partially reversed by VX-765 (HY-13205). RR-171 inhibits the viability, proliferation and colony formation of pancreatic cancer cells, with low cytotoxicity against normal cells. RR-171 downregulates the expression of Ki-67 and PCNA in tumor tissues in vivo, with favorable biosafety. RR-171 can be used in studies related to pancreatic cancer.

YW2036 (compound 2a) is a potent Wnt/β-Catenin signaling pathway inhibitor with an IC₅₀ value of 637 nM. YW2036 can be used in research of colorectal cancer (CRC).

hsBCL9CT-24 is a Wnt/β-catenin (b-cat) pathway inhibitor with potent anti-tumor effect. hsBCL9CT-24 reactivates anti-cancer immune response suppressed by the oncogenic Wnt pathway and can be utilized for cancer research.

PI3Kα-IN-16 (Z86) is a novel PI3Kα inhibitor with an IC₅₀ value of 4.28 μM. PI3Kα-IN-16 has potent inhibitory efficiency on PI3K-mediated CRCs growth and migration. PI3Kα-IN-16 also inhibits the Wnt signaling pathway.

CDK8-IN-11 hydrochloride is a potent and selective CDK8 inhibitor with an IC₅₀ value of 46 nM. CDK8-IN-11 hydrochloride inhibits WNT/β-catenin signaling pathway. CDK8-IN-11 hydrochloride can be used in the research of colon cancer.

β-Catenin modulator-9 (Compound IIa-2075) is a β-Catenin modulator. β-Catenin modulator-9 specifically targets the activity of the stable β-catenin pool and inhibits the Wnt signaling pathway. β-Catenin modulator-9 can be used in cancer-related research.

Wnt/β-catenin-in-1 (compounds 17) is a Wnt/β-catenin signaling pathway inhibitor. Wnt/β-catenin-IN-1 can induce apoptosis of colon cancer cells, has broad-spectrum anticancer activity, and can be used for the reseach of a variety of solid tumors.

Tizanidine-d₄ hydrochloride is deuterium labeled Tizanidine hydrochloride (HY-B0194A). Tizanidine hydrochloride, a skeletal muscle relaxant, is an orally effective central α₂-adrenoceptor agonist (IC₅₀ = 6.9 nmol). Tizanidine hydrochloride 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 hydrochloride has anti-injury activity and can inhibit gastrointestinal (GI) transport. Tizanidine hydrochloride 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 hydrochloride can be used to treat spasticity caused by diseases such as multiple sclerosis (MS), stroke, and spinal cord injury (SCI).

Wnt/β-catenin-IN-7 (Example 3) is a Wntsignal inhibitor with an IC₅₀ of 0.15 μM. Wnt/β-catenin-IN-7 can be used in the research of cancer and fibrosis.

Pizotyline-d₃ (BC-105-d₃) is the d₃-labeled Pizotifen (HY-B0115). 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.

1(R),2(S)-epoxy Cannabidiol (Compound 2a) is a structural analogue of phytocannabinoidsphytocannabinoids. 1(R),2(S)-epoxy Cannabidiol exhibits potent inhibitory activity against Wnt/β-catenin pathway. 1(R),2(S)-epoxy Cannabidiol is promising for research of neuroprotective agents.