Wnt/beta-catenin Inhibitors

Cat.No.	Product Name	Information	Product Use Citations
S2662	ICG-001	ICG-001 antagonizes Wnt/β-catenin/TCF-mediated transcription and specifically binds to CREB-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300. ICG-001 induces apoptosis.	Cancer Discov, 2025, 10.1158/2159-8290.CD-25-0629 Adv Sci (Weinh), 2025, 12(40):e05702 Cell Rep Med, 2025, 6(2):101927
S7086	IWR-1-endo	IWR-1-endo (endo-IWR 1, IWR-1) is a Wnt pathway inhibitor with IC50 of 180 nM in L-cells expressing Wnt3A, induces Axin2 protein levels and promotes β-catenin phosphorylation by stabilizing Axin-scaffolded destruction complexes.	Nat Biotechnol, 2025, 10.1038/s41587-025-02833-3 Circulation, 2025, 151(20):1436-1448 Nat Commun, 2025, 16(1):5529
S7085	IWP-2	IWP-2 is an inhibitor of Wnt processing and secretion with IC50 of 27 nM in a cell-free assay, selective blockage of Porcn-mediated Wnt palmitoylation, does not affect Wnt/β-catenin in general and displays no effect against Wnt-stimulated cellular responses. IWP-2 specifically inhibits CK1δ.	Sci Bull (Beijing), 2025, S2095-9273(25)00472-4 Nat Commun, 2025, 16(1):1999 Nat Commun, 2025, 16(1):4688
S8429	PNU-74654	PNU-74654 disrupts the Wnt signaling pathway via inhibition of the interaction (KD50=450 nM) between β-catenin and Tcf4.	Am J Cancer Res, 2025, 15(7):2949-2969 Viruses, 2025, 17(3)400 Cell Rep, 2024, 43(7):114414
S8129	Salinomycin (Procoxacin)	Salinomycin, traditionally used as an anti-coccidial drug, has recently been shown to possess anti-cancer and anti-cancer stem cell (CSC) effects.	Haematologica, 2025, 10.3324/haematol.2025.288464 Cell Death Discov, 2024, 10(1):9 Biomolecules, 2023, 13(6)965
S7484	FH535	FH535 is a Wnt/β-catenin signaling inhibitor and also a dual PPARγ and PPARδ antagonist.	Int J Biol Sci, 2024, 20(6):2323-2338 Gastroenterology, 2023, S0016-5085(23)00114-2 Gastroenterology, 2023, 164(6):990-1005
S8474	LF3	LF3 is a specific inhibitor of canonical Wnt signaling by disrupting the interaction between β-catenin and TCF4 with an IC50 less than 2 μM.	Colloids Surf B Biointerfaces, 2025, 251:114586 Cell Mol Biol Lett, 2024, 29(1):103 Elife, 2024, 12RP86978
S8327	KYA1797K	KYA1797K is a highly potent and selective Wnt/β-catenin inhibitor with IC50 of 0.75 µM (TOPflash assay).	Mil Med Res, 2025, 12(1):83 Gut Microbes, 2023, 15(1):2192501 Exp Biol Med (Maywood), 2023, 248(23):2210-2218
S7096	KY02111	KY02111 promotes differentiation of hPSCs to cardiomyocytes by inhibiting Wnt signaling, may act downstream of APC and GSK3β.	Front Pharmacol, 2022, 13:889713 Sci Rep, 2022, 12(1):7 Stem Cell Res, 2022, 60:102686
S6901	MSAB	MSAB is a selective inhibitor of Wnt/β-catenin signaling that binds to β-catenin, promoting its degradation, and specifically downregulates Wnt/β-catenin target genes. This compound shows potent anti-tumor effects.	Bioact Mater, 2025, 46:259-272 Oncogene, 2024, 10.1038/s41388-024-03008-1 Cells, 2024, 13(19)1663
S8761	Adavivint (SM04690)	Adavivint (SM04690, Lorecivivint) is a potent and specific inhibitor of canonical Wnt signaling with an EC50 of 19.5 nM for inhibiting the TCF/LEF reporter. This compound is ∼150- to 500-fold more potent than other known Wnt inhibitors across multiple cellular assays.	Commun Biol, 2024, 7(1):1649 Elife, 2023, 12RP88508 Int J Mol Sci, 2023, 24(6)5252
S3842	Isoquercitrin	Isoquercitrin (Hirsutrin, 3-Glucosylquercetin, Quercetin 3-o-glucopyranoside), a flavonoid compound with anticancer activity isolated from Bidens bipinnata L, is an inhibitor of Wnt/β-catenin that acts downstream of the β-catenin nuclear translocation.	Cancers, August 20, 2021, 4200 Molecules, 2025, 30(6)1394 Commun Biol, 2023, 6(1):79
S8704	iCRT14	iCRT14 is a β-catenin/Tcf inhibitor with a Ki value of 54 ± 5.2 μM in homogeneous fluorescence polarization (FP) assay.	Biol Open, 2025, 14(9)bio062175 Nature Communications, 2024, 6737 Bone Research, 2023, 18
S7981	CCT251545	CCT251545 is a potent, orally bioavailable inhibitor of WNT signaling with IC50 of 5 nM in 7dF3 cells. This compound also acts as a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.	eLife, 2025, e100197 Science, 2022, 378(6620):eabn5647 Pathol Oncol Res, 2022, 28:1610273
S8248	IQ-1	IQ-1 enables Wnt/β-catenin-driven expansion of mouse ESCs and prevents spontaneous differentiation, Maintains embryonic stem cell (ESC) pluripotency in Wnt3a-treated cells and prevents PP2A/Nkd interaction.	Haematologica, 2023, 490-501 Haematologica, 2022, 10.3324/haematol.2022.280760 Neoplasia, 2021, 1-11
S6745	JW55	JW55 is a potent and selective inhibitor of the canonical Wnt pathway that functions via inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2).	Cell Discov, 2024, 10(1):39 Oncotarget, 2021, 12(7):674-685 Chin J Integr Med, 2021, 10.1007/s11655-021-3282-0
S9965	M435-1279	M435-1279 is a UBE2T inhibitor, inhibiting the Wnt/β-catenin signaling pathway hyperactivation through blocking UBE2T-mediated degradation of RACK1.	Journal for ImmunoTherapy of Cancer, 2025, e010782 Drug Des Devel Ther, 2023, 17:1357-1369 Drug Design, Development and Therapy, 2023, 1357-1369
S9416	Triptonide	Triptonide, isolated from the roots of Tripterygium wilfordii, can effectively inhibit canonical Wnt/β-catenin signaling by targeting the downstream C-terminal transcription domain of β-catenin or a nuclear component associated with β-catenin. It is also an antineoplastic agent, an anti-inflammatory agent and an immunosuppressive agent.	Military Medical Research, April 29, 2024, 27 Mil Med Res, 2024, 11(1):27 iScience, 2024, 27(10):110862
E1731	JW74	JW74 is a specific inhibitor of the canonical Wnt signaling with IC50 790 nM in the ST-Luc assay. It inhibit the growth of tumor cells in both mouse xenograft model of colorectal cancer and in Apc^Min mice.	Nature Communications, October 09, 2024, 15(1) Communications Biology, February 20, 2023, 197 Bioactive Materials, 2023, 100670
S8233	Prodigiosin	Prodigiosin is a natural red pigment produced by numerous bacterial species which can inhibit Wnt/β-catenin pathway.	Cell Chemical Biology, 2019, 1133-1142.e4
E0033	IWP-4	IWP-4 is a potent Wnt/β-catenin signaling pathway inhibitor with an IC50 of 25 nM.	Oncogene, 2023, 42(35):2629-2640
E1486	Zamaporvint (RXC004)	Zamaporvint (RXC004) is an orally active and selective inhibitor of Wnt. This compound targets membrane-bound o-acyltransferase Porcupine and inhibits Wnt ligand palmitoylation, secretion, and pathway activation. It exhibits potent antiproliferative effects in Wnt ligand-dependent colorectal and pancreatic cell lines and possesses multiple antitumor mechanisms.
E0769	Ginsenoside Rh4	Ginsenoside Rh4 is an important active ingredient of traditional Chinese medicine ginseng, which has been shown to inhibit Wnt/β-Catenin, JAK2/STAT3, TGF-β/Smad2/3 and other signaling pathways.
E6057^New	Pamidronate disodium pentahydrate	Pamidronate disodium pentahydrate is a nitrogen-containing bisphosphonate and used to prevent bone loss due to steroid use like glucocorticoid-induced low bone mineral density in children or to inhibit calcium release from bone by impairing osteoclast-mediated bone resorption. It also inhibits the Wnt/β-catenin signaling pathway that controls osteogenic differentiation in bone marrow mesenchymal stem cells (BMMSCs).
S1180	XAV-939	XAV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM in cell-free assays, regulates axin levels and does not affect CRE, NF-κB or TGF-β.	Nat Biotechnol, 2025, 10.1038/s41587-025-02649-1 Nat Cell Biol, 2025, 27(8):1240-1255 Nat Cell Biol, 2025, NONE
S2788	Capmatinib (INC280)	Capmatinib is a novel, ATP-competitive inhibitor of c-MET with IC50 of 0.13 nM in a cell-free assay, inactive against RONβ, as well as EGFR and HER-3. Capmatinib (INCB28060) inhibits Wnt/β-catenin and EMT signaling pathways and induces apoptosis in diffuse gastric cancer positive for c-MET amplification. Phase 1.	Mol Cancer, 2025, 24(1):272 Cell Rep Med, 2025, 6(9):102335 J Biomed Sci, 2025, 32(1):94
S8392	NCB-0846	NCB-0846 is a novel, orally small-molecule Wnt inhibitor that inhibits TNIK (TRAF2 and NCK-Interacting Kinase, MAP4K7) with an IC50 value of 21 nM.	Molecular Cancer Therapeutics, August 1, 2024, 23(8):1201-1211 Nat Commun, 2024, 15(1):2551 Genes Dis, 2024, 11(3):100997
S6898	RCM-1	RCM-1 is a nontoxic inhibitor of Forkhead box M1 (FOXM1) that suppresses goblet cell metaplasia and prevents IL-13 and STAT6 signaling in allergen-exposed mice. This compound decreases carcinogenesis and nuclear β-catenin.	Gut, 2025, gutjnl-2025-335163 Parasit Vectors, 2025, 18(1):100 bioRxiv, 2025, 2025.05.25.655133
S3238	Resibufogenin	Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. This compound exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. It induces apoptosis and caspase-3 and caspase-8 activity. This chemical increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.	bioRxiv, 2025, 2025.07.17.665404 Research Square, 2024, 10.21203/rs.3.rs-3790060/v1 Phytomedicine, 2022, 102:154182
E1348	E7386	E-7386 is a selective inhibitor which inhibits interaction between CBP/beta-catenin with IC50 value of 0.0484 μM in HEK293 cells.	Adv Sci (Weinh), 2024, 11(35):e2308417 Cell Rep, 2024, 43(8):114532 Newcastle University eTheses, 2024, 129
S7490	WIKI4	WIKI4 is a novel Tankyrase inhibitor with IC50 of 15 nM for TNKS2, and leads to inhibition of Wnt/beta-catenin signaling.	Sci Rep, 2022, 12(1):7 Carcinogenesis, 2020, 41(7):993-1004 Nat Commun, 2019, 10(1):4363
E2376	KY-05009	KY-05009 is an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a Ki of 100 nM, which inhibits the protein expression of TNIK and transcriptional activity of Wnt target genes and induces apoptosis in cancer cells.	Front Public Health, 2025, 13:1582860 Frontiers in Public Health, 2025, 1582860
E1069	M2912	M2912 (MSC2504877) is a very potent TNKS1/TNKS2 inhibitor (IC50=0.6 nM for TNKS1) with exquisite selectivity over other PARP family enzymes and favorable compound properties. This inhibitor potently modulates the Wnt/β-catenin pathway by elevating the levels of axin2 (EC50=17 nM) and tankyrase in DLD1 cells in a dose-dependent manner resulting in reduced cellular Wnt reporter activity.
S5554	Lanatoside C	Lanatoside C is a cardiac glycoside with antiviral and anti-tumor activity. This compound induces G2/M cell cycle arrest and induces autophagy and apoptosis via attenuating MAPK, Wnt, JAK-STAT, and PI3K/AKT/mTOR signaling pathways.