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The Wnt signaling pathways are a group of signal transduction pathways made of proteins that pass signals from outside of a cell through cell surface receptors to the inside of the cell. Three Wnt signaling pathways have been characterized: the canonical Wnt pathway, the noncanonical planar cell polarity pathway, and the noncanonical Wnt/calcium pathway. All three Wnt signaling pathways are activated by the binding of a Wnt-protein ligand to a Frizzled family receptor, which passes the biological signal to the protein Dishevelled inside the cell. The canonical Wnt pathway leads to regulation of gene transcription, the noncanonical planar cell polarity pathway regulates the cytoskeleton that is responsible for the shape of the cell, and the noncanonical Wnt/calcium pathway regulates calcium inside the cell. The clinical importance of Wnt signaling pathway has been demonstrated by mutations that lead to a variety of diseases, including breast and prostate cancer, glioblastoma, type II diabetes.

Cat. No.	Product Name	CAS No.	Information
H9627	ARUK 3001185	2411969-39-4	ARUK 3001185 is a potent, selective, brain-penetrant inhibitor of Wnt-deactivating enzyme Notum carboxylesterase activity with IC50 of 6.7 nM in OPTS biochemical assay;ARUK 3001185 restored Wnt signaling in the presence of Notum (EC50 110 nM) in a in a cell-based TCF/LEF (Luciferase) reporter assay.ARUK 3001185 demonstrated high selectivity against a panel of serine hydrolases, kinases, and representative drug targets.ARUK 3001185 displayed good brain penetration suitable for oral dosing in rodent models of disease.
H9513	KY-02327	2093407-25-9	KY-02327 is a metabolically stabilized KY-02061 analog, is a potent Dishevelled (Dvl)-CXXC5 interaction inhibitor. KY-02327 shows an activating effect on the Wnt/β-catenin pathway, resulting in promotion of osteoblast differentiation.
H9327	Foscenvivint	1422253-38-0	Foscenvivint is a potent, specific inhibitor of the canonical Wnt signaling pathway in cancer stem cells with potential antineoplastic activity. Wnt signaling pathway inhibitor PRI-724 specifically inhibits the recruiting of beta-catenin with its coactivator CBP (the binding protein of the cAMP response element-binding protein CREB); together with other transcription factors beta-catenin/CBP binds to WRE (Wnt-responsive element) and activates transcription of a wide range of target genes of Wnt/beta-catenin signaling.
H8892	Tilpisertib	2065153-41-3	Tilpisertib is a serine/threonine kinase inhibitor.
H8848	Ipivivint	1481617-15-5	Ipivivint is a potent inhibiteur de la voie Wnt.
H8810	Cirtuvivint	2143917-62-6	Cirtuvivint is a novel Wnt pathway inhibitor.
H8327	Wntepane 1	1314885-81-8	Wntepane 1 is a small-molecule activator of the Wnt pathway that modulates the van-Gogh-like receptor 1 (Vangl1), activates Wnt signaling with EC50 of 1.8 uM in the reporter gene assay; it is likely that Wntepane-1 interacts with Vangl1 (and possibly Vangl2 as well) and thereby at least partially liberates and restores the signal transducing activity of Dsh; an advantageous tool for the study of biological processes mediated by Vangl1.
H8326	Wnt-p53 inhibitor compound 2	1448427-02-8	Wnt-p53 inhibitor compound 2 is a novel inhibitor targets both Wnt signaling and ATM/p53, potently inhibits Wnt transcription (IC50=11 nM) and p53 transcription (EC50=1.9 nM); decreases HCT-116 CRC cell viability (IC50=10 nM) and proliferation (IC50=8 nM), decreases DLD-1, SW480 and 10.1 cancer cell viability (IC50=12, 27 and 41 nM) and proliferation (IC50=18,15 and 13 nM); compound 2 potently activates apoptosis of HCT-116, DLD-1 and SW480 cells (EC50=13, 15 and 18 nM) in a p53-dependent manner; inhibits cell migration and invasion in HCT-116 at 20-200 nM, also modulates mitotic stress signaling, leading to both inhibition of Wnt responsiveness and stabilization and activation of p53 to cause cell cycle arrest; induces cell death and inhibits tumor growth in mouse xenografts (20 mg/kg/day, i.p.), without acute cytotoxicity nor toxicity.
H8325	QS-11	944328-88-5	A small molecule inhibitor of GTPase activating protein of ADP-ribosylation factor 1 (ARFGAP1) with Kd of 620 nM, synergizes the Wnt/beta-catenin signaling; synergizes with Wnt-3a in activating Wnt signaling through ARF activation (EC50=0.5 uM), increases levels of nuclear β-catenin and inhibits the migration of MDA-MB-231 cells with IC80 of 2.5 uM.
H8324	Prodigiosin	82-89-3	Prodigiosin is a natural red pigment produced by numerous bacterial species, has exhibited promising anticancer activity; a potent inhibitor of Wnt/β-catenin pathway by targeting multiple sites of this pathway, including LRP6, Dishevelled (DVL), and GSK3β; decreases phosphorylation of LRP6, DVL2, and GSK3β and suppressed β-catenin-stimulated Wnt target gene expression, including expression of cyclin D1, in breast cancer cells; slows tumor progression in vivo; restores p53 and activates p73 via regualtion of c-Jun in colorectal cancer stem cells.

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