Wnt/beta-catenin

Isoform-selective Products

Signaling Pathway

Wnt/beta-catenin Signaling Pathway

Wnt/beta-catenin Products

  • All (51)
  • Wnt/beta-catenin Inhibitors (33)
  • Wnt/beta-catenin Activators (10)
  • Wnt/beta-catenin Antagonists (2)
  • Wnt/beta-catenin Agonists (3)
  • Wnt/beta-catenin Modulators (3)
  • New Wnt/beta-catenin Products
Catalog No. Product Name Information Product Use Citations Product Validations
S1263 Laduviglusib (CHIR-99021) Laduviglusib (CHIR-99021, CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs. CHIR99021 functions as a Wnt/β-catenin activator and induces autophagy.
Nat Cancer, 2024, 10.1038/s43018-023-00716-7
Circ Res, 2024, 134(5):482-501
Bioact Mater, 2024, 31:463-474
S2924 Laduviglusib (CHIR-99021) HCl Laduviglusib (CHIR-99021; CT99021) HCl is hydrochloride of CHIR-99021, which is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs Cdc2 and ERK2. CHIR-99021 is a potent pharmacological activators of the Wnt/beta-catenin signaling pathway. CHIR-99021 significantly rescues light-induced autophagy and augments GR, RORα and autophagy-related proteins.
Nat Cancer, 2024, 10.1038/s43018-023-00716-7
Nat Commun, 2024, 15(1):1285
Nat Commun, 2024, 15(1):668
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.
Adv Sci (Weinh), 2024, 11(1):e2303637
ACS Omega, 2024, 9(7):7782-7792
Heliyon, 2024, 10(1):e23057
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.
Int J Biol Sci, 2024, 20(3):848-863
Mol Metab, 2024, 79:101841
Heliyon, 2024, 10(1):e23690
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 Commun, 2024, 15(1):167
Stem Cell Reports, 2024, 19(2):196-210
Oncol Rep, 2024, 51(2)22
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.
Nat Commun, 2024, 15(1):1351
Nat Commun, 2024, 15(1):167
Cell Res, 2023, 10.1038/s41422-023-00846-8
S2788 Capmatinib 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.
J Thorac Oncol, 2023, 10.1016/j.jtho.2023.10.017
J Exp Clin Cancer Res, 2023, 10.1186/s13046-023-02866-z
NPJ Precis Oncol, 2023, 7(1):107
S8320 SKL2001 SKL2001 is a novel agonist of the Wnt/β-catenin pathway. It disrupts the Axin/β-catenin interaction.
Nat Cancer, 2024, 10.1038/s43018-023-00716-7
Int J Biol Sci, 2024, 20(3):848-863
Cell Death Dis, 2023, 14(10):696
S8178 BML-284 (Wnt agonist 1) BML-284 (Wnt agonist 1) is a cell permeable Wnt signaling pathway activator, which induces β-catenin- and TCF-dependent transcriptional activity with EC50 of 0.7 μM.
Cell Rep Med, 2023, 4(1):100881
Mol Med, 2023, 29(1):101
Mol Med, 2023, 29(1):101
S8968 PRI-724 PRI-724 (C-82 prodrug, ICG-001 analog) is a potent and specific inhibitor that disrupts the interaction of β-catenin and CBP.
Nat Commun, 2023, 14(1):4671
Cell Rep, 2023, 42(7):112804
J Transl Med, 2023, 21(1):50
S8129 Salinomycin (from Streptomyces albus) Salinomycin, traditionally used as an anti-coccidial drug, has recently been shown to possess anti-cancer and anti-cancer stem cell (CSC) effects.
Cell Death Discov, 2024, 10(1):9
Biomolecules, 2023, 13(6)965
Oncotarget, 2023, 14:879-889
S7484 FH535 FH535 is a Wnt/β-catenin signaling inhibitor and also a dual PPARγ and PPARδ antagonist.
Gastroenterology, 2023, S0016-5085(23)00114-2
Gastroenterology, 2023, 164(6):990-1005
Cell Death Dis, 2022, 13(5):493
S8429 PNU-74654 PNU-75654 disrupts the Wnt signaling pathway via inhibition of the interaction (KD50=450 nM) between β-catenin and Tcf4.
Cell Biol Int, 2023, 47(7):1259-1266
JCI Insight, 2022, e158855
PLoS Pathog, 2022, 18(3):e1010354
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.
Redox Biol, 2023, 10.1016/j.redox.2023.102942
Redox Biol, 2023, 68:102942.
J Exp Clin Cancer Res, 2023, 42(1):150
S8327 KYA1797K KYA1797K is a highly potent and selective Wnt/β-catenin inhibitor with IC50 of 0.75 µM (TOPflash assay).
Gut Microbes, 2023, 15(1):2192501
Exp Biol Med (Maywood), 2023, 248(23):2210-2218
Cardiovasc Diagn Ther, 2023, 13(3):523-533
S7954 CP21R7 CP21R7 is a potent and selective GSK-3β inhibitor that can potently activate canonical Wnt signalling.
Cell, 2022, 185(14):2523-2541.e30
Sci Rep, 2022, 12(1):7
ACS Nano, 2021, 10.1021/acsnano.1c06452
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
S8647 iCRT3 iCRT3 is an antagonist of Wnt/β-catenin signaling with an IC50 of 8.2 nM in the Wnt responsive STF16-luc reporter assays.
EMBO J, 2022, 41(15):e110218
EMBO Mol Med, 2022, e14990
Gastroenterology, 2021, S0016-5085(21)03489-2
S5992 Heparan Sulfate Heparan sulfate (HS, Heparitin sulfate, Alpha-idosane, HHS 5, N-Acetylheparan Sulfate, Suleparoid, Tavidan), a constituent of HS proteoglycans (HSPGs), is a linear polysaccharide present on the cell surface. Heparan sulfate influences the binding affinity of intestinal epithelium cells (IECs) to Wnt, thereby promoting activation of canonical Wnt signaling and facilitating regeneration of small intestinal crypts after epithelial injury.
Mol Genet Genomics, 2022, 297(2):397-405
PeerJ, 2022, 10:e14003
Glycobiology, 2019, 29-8:572-581
S7421 CGP 57380 CGP 57380 is a potent MNK1 inhibitor with IC50 of 2.2 μM, exhibiting no inhibitory activity on p38, JNK1, ERK1 and -2, PKC, or c-Src-like kinases. CGP 57380 upregulates β-catenin and potentiates radiation-induced apoptosis.
Cell Commun Signal, 2023, 21(1):107
Fundam Clin Pharmacol, 2022, 10.1111/fcp.12759
J Cancer, 2020, 11(4):990-996
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. It is ∼150- to 500-fold more potent than the other known Wnt inhibitors across multiple cellular assays.
Int J Mol Sci, 2023, 24(6)5252
bioRxiv, 2023, 2023.04.19.537449
PLoS Pathog, 2022, 18(3):e1010354
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. MSAB shows potent anti-tumor effects.
BMC Mol Cell Biol, 2023, 24(1):4
Eur Arch Otorhinolaryngol, 2023, 280(1):399-408
Clin Transl Med, 2022, 12(2):e684
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.
Commun Biol, 2023, 6(1):79
FASEB J, 2022, 36(7):e22369
Cancers (Basel), 2021, 13(16)4200
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.
Sci Rep, 2022, 12(1):7
Adv Biol (Weinh), 2022, 6(8):e2200030
Neoplasia, 2019, 21(4):389-400
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, 2022, 10.3324/haematol.2022.280760
Neoplasia, 2020, 23(1):1-11
Cell Mol Life Sci, 2019, 76(14):2817-2832
S8704 iCRT14 iCRT14 is a β-catenin/Tcf inhibitor with a Ki value of 54 ± 5.2 μM in homogeneous fluorescence polarization (FP) assay.
Bone Res, 2023, 11(1):18
mBio, 2023, e0168823.
PLoS Pathog, 2022, 18(3):e1010354
S7981 CCT251545 CCT251545 is a potent, orally bioavailable inhibitor of WNT signaling with IC50 of 5 nM in 7dF3 cells. CCT251545 also act as a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
Science, 2022, 378(6620):eabn5647
Pathol Oncol Res, 2022, 28:1610273
Front Cell Dev Biol, 2020, 8:408
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
S7914 Isoxazole 9 (ISX-9) Isoxazole 9 (Isx-9) is a synthetic promotor of adult neurogenesis by triggering neuronal differentiation of adult neural stem/precursor cells (NSPCs). Isoxazole 9 (Isx-9) activates multiple pathways including TGF-β induced epithelial–mesenchymal transition (EMT) signaling, canonical and non-canonical Wnt signaling at different stages of cardiac differentiation.
Commun Biol, 2022, 5(1):750
Front Cell Dev Biol, 2021, 9:728352
Front Cell Dev Biol, 2021, 9:728352
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).
Oncotarget, 2021, 12(7):674-685
Chin J Integr Med, 2021, 10.1007/s11655-021-3282-0
S3630 Methyl Vanillate Methyl Vanillate, one of the ingredients in Hovenia dulcis Thunb, activates the Wnt/β-catenin pathway and induces osteoblast differentiation in vitro.
Sci Rep, 2022, 12(1):7
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. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.
Research Square, 2024, 10.21203/rs.3.rs-3790060/v1
Phytomedicine, 2022, 102:154182
S9965 M435-1279 M435-1279 is a UBE2T inhibitor, inhibiting the Wnt/β-catenin signaling pathway hyperactivation through blocking UBE2T-mediated degradation of RACK1.
Drug Des Devel Ther, 2023, 17:1357-1369
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. RCM-1 decreases carcinogenesis and nuclear β-catenin.
Front Immunol, 2022, 13:863034
S5815 WAY-316606 WAY-316606, a specific antagonist of SFRP1, functions as an activator of canonical Wnt/β-catenin signalling in the human hair bulb.
Stem Cells Transl Med, 2024, szae006
J Bone Miner Res, 2021, 10.1002/jbmr.4435
S9828 WAY-262611 WAY-262611 (BML-WN110, Compound 5) is a beta-catenin (β-Catenin) agonist that increases bone formation rate with EC50 of 0.63 μM in TCF-Luciferase assay. WAY-262611 is also an inhibitor of dickkopf 1 (DKK1).
J Orthop Surg Res, 2023, 18(1):751
Nat Commun, 2022, 13(1):7194
E1731New 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 ApcMin mice.
Commun Biol, 2023, 6(1):197
S6961 Foxy-5 Foxy-5, a Wnt-5a mimicking hexapeptide, is a WNT signalling pathway modulator potentially for the treatment of metastatic breast cancer, prostate cancer and colorectal cancer.
CNS Neurosci Ther, 2023, 10.1111/cns.14099
S3223 L-Quebrachitol L-Quebrachitol (L-QCT), a natural product isolated from many plants, promotes proliferation and cell DNA synthesis. L-Quebrachitol upregulates bone morphogenetic protein-2 (BMP-2) and runt-related transcription factor-2 (Runx2) and regulatory genes associated with mitogen-activated protein kinase (MAPK) and Wnt/β-catenin signaling pathway, while down-regulating the receptor activator of the nuclear factor-κB(NF-κB) ligand (RANKL) mRNA level.
E1486New Zamaporvint (RXC004) Zamaporvint (RXC004) is an orally active and selective inhibitor of Wnt. It targets membrane-bound o-acyltransferase Porcupine and inhibits Wnt ligand palmitoylation, secretion, and pathway activation. RXC004 exhibits potent antiproliferative effects in Wnt ligand-dependent colorectal and pancreatic cell lines and possesses multiple antitumor mechanisms.
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.
S0733 Tegatrabetan (BC-2059) Tegatrabetan (BC2059,Tegavivint) is an antagonist of β-Catenin. Tegatrabetan (BC2059) treatment disrupts the binding of β-catenin with the scaffold protein transducin β-like 1 (TBL1) and proteasomal degradation and declines in the nuclear levels of β-catenin.
S5554 Lanatoside C Lanatoside C is a cardiac glycoside with antiviral and anti-tumor activity. Lanatoside C induces G2/M cell cycle arrest and induces autophagy and apoptosis via attenuating MAPK, Wnt, JAK-STAT, and PI3K/AKT/mTOR signaling pathways.
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.
E0072 Indirubin-3′-oxime Indirubin-3′-oxime (IDR3O, I3O) is an indirubin analogue that shows favorable inhibitory activity targeting GSK-3β and CDKs. Indirubin-3′-oxime also inhibits JNKs with IC50s of 0.8 μM, 1.4 μM, and 1.0 μM for JNK1, JNK2, and JNK3, respectively. Indirubin-3′-oxime activates Wnt/β-catenin signaling and inhibits adipocyte differentiation and obesity.
S8233 Prodigiosin Prodigiosin is a natural red pigment produced by numerous bacterial species which can inhibit Wnt/β-catenin pathway.
S6085 KY19382 (A3051) KY19382 (A3051) is a Wnt/β-catenin signalling activator through inhibitory effects on both CXXC5–DVL interaction and GSK3β activity with IC50s of 19 nM and 10 nM, respectively.
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.
E0033 IWP-4

IWP-4 is a potent Wnt/β-catenin signaling pathway inhibitor with an IC50 of 25 nM.

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.
S0458 KY1220 KY1220 is a small molecule that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway with IC50 of 2.1 μM in HEK293 reporter cells.
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.
Adv Sci (Weinh), 2024, 11(1):e2303637
ACS Omega, 2024, 9(7):7782-7792
Heliyon, 2024, 10(1):e23057
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.
Int J Biol Sci, 2024, 20(3):848-863
Mol Metab, 2024, 79:101841
Heliyon, 2024, 10(1):e23690
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 Commun, 2024, 15(1):167
Stem Cell Reports, 2024, 19(2):196-210
Oncol Rep, 2024, 51(2)22
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.
Nat Commun, 2024, 15(1):1351
Nat Commun, 2024, 15(1):167
Cell Res, 2023, 10.1038/s41422-023-00846-8
S2788 Capmatinib 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.
J Thorac Oncol, 2023, 10.1016/j.jtho.2023.10.017
J Exp Clin Cancer Res, 2023, 10.1186/s13046-023-02866-z
NPJ Precis Oncol, 2023, 7(1):107
S8968 PRI-724 PRI-724 (C-82 prodrug, ICG-001 analog) is a potent and specific inhibitor that disrupts the interaction of β-catenin and CBP.
Nat Commun, 2023, 14(1):4671
Cell Rep, 2023, 42(7):112804
J Transl Med, 2023, 21(1):50
S8129 Salinomycin (from Streptomyces albus) Salinomycin, traditionally used as an anti-coccidial drug, has recently been shown to possess anti-cancer and anti-cancer stem cell (CSC) effects.
Cell Death Discov, 2024, 10(1):9
Biomolecules, 2023, 13(6)965
Oncotarget, 2023, 14:879-889
S7484 FH535 FH535 is a Wnt/β-catenin signaling inhibitor and also a dual PPARγ and PPARδ antagonist.
Gastroenterology, 2023, S0016-5085(23)00114-2
Gastroenterology, 2023, 164(6):990-1005
Cell Death Dis, 2022, 13(5):493
S8429 PNU-74654 PNU-75654 disrupts the Wnt signaling pathway via inhibition of the interaction (KD50=450 nM) between β-catenin and Tcf4.
Cell Biol Int, 2023, 47(7):1259-1266
JCI Insight, 2022, e158855
PLoS Pathog, 2022, 18(3):e1010354
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.
Redox Biol, 2023, 10.1016/j.redox.2023.102942
Redox Biol, 2023, 68:102942.
J Exp Clin Cancer Res, 2023, 42(1):150
S8327 KYA1797K KYA1797K is a highly potent and selective Wnt/β-catenin inhibitor with IC50 of 0.75 µM (TOPflash assay).
Gut Microbes, 2023, 15(1):2192501
Exp Biol Med (Maywood), 2023, 248(23):2210-2218
Cardiovasc Diagn Ther, 2023, 13(3):523-533
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
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. It is ∼150- to 500-fold more potent than the other known Wnt inhibitors across multiple cellular assays.
Int J Mol Sci, 2023, 24(6)5252
bioRxiv, 2023, 2023.04.19.537449
PLoS Pathog, 2022, 18(3):e1010354
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. MSAB shows potent anti-tumor effects.
BMC Mol Cell Biol, 2023, 24(1):4
Eur Arch Otorhinolaryngol, 2023, 280(1):399-408
Clin Transl Med, 2022, 12(2):e684
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.
Commun Biol, 2023, 6(1):79
FASEB J, 2022, 36(7):e22369
Cancers (Basel), 2021, 13(16)4200
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.
Sci Rep, 2022, 12(1):7
Adv Biol (Weinh), 2022, 6(8):e2200030
Neoplasia, 2019, 21(4):389-400
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, 2022, 10.3324/haematol.2022.280760
Neoplasia, 2020, 23(1):1-11
Cell Mol Life Sci, 2019, 76(14):2817-2832
S8704 iCRT14 iCRT14 is a β-catenin/Tcf inhibitor with a Ki value of 54 ± 5.2 μM in homogeneous fluorescence polarization (FP) assay.
Bone Res, 2023, 11(1):18
mBio, 2023, e0168823.
PLoS Pathog, 2022, 18(3):e1010354
S7981 CCT251545 CCT251545 is a potent, orally bioavailable inhibitor of WNT signaling with IC50 of 5 nM in 7dF3 cells. CCT251545 also act as a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
Science, 2022, 378(6620):eabn5647
Pathol Oncol Res, 2022, 28:1610273
Front Cell Dev Biol, 2020, 8:408
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
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).
Oncotarget, 2021, 12(7):674-685
Chin J Integr Med, 2021, 10.1007/s11655-021-3282-0
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. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.
Research Square, 2024, 10.21203/rs.3.rs-3790060/v1
Phytomedicine, 2022, 102:154182
S9965 M435-1279 M435-1279 is a UBE2T inhibitor, inhibiting the Wnt/β-catenin signaling pathway hyperactivation through blocking UBE2T-mediated degradation of RACK1.
Drug Des Devel Ther, 2023, 17:1357-1369
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. RCM-1 decreases carcinogenesis and nuclear β-catenin.
Front Immunol, 2022, 13:863034
E1731New 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 ApcMin mice.
Commun Biol, 2023, 6(1):197
E1486New Zamaporvint (RXC004) Zamaporvint (RXC004) is an orally active and selective inhibitor of Wnt. It targets membrane-bound o-acyltransferase Porcupine and inhibits Wnt ligand palmitoylation, secretion, and pathway activation. RXC004 exhibits potent antiproliferative effects in Wnt ligand-dependent colorectal and pancreatic cell lines and possesses multiple antitumor mechanisms.
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. Lanatoside C induces G2/M cell cycle arrest and induces autophagy and apoptosis via attenuating MAPK, Wnt, JAK-STAT, and PI3K/AKT/mTOR signaling pathways.
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.
S8233 Prodigiosin Prodigiosin is a natural red pigment produced by numerous bacterial species which can inhibit Wnt/β-catenin pathway.
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.
E0033 IWP-4

IWP-4 is a potent Wnt/β-catenin signaling pathway inhibitor with an IC50 of 25 nM.

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.
S1263 Laduviglusib (CHIR-99021) Laduviglusib (CHIR-99021, CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs. CHIR99021 functions as a Wnt/β-catenin activator and induces autophagy.
Nat Cancer, 2024, 10.1038/s43018-023-00716-7
Circ Res, 2024, 134(5):482-501
Bioact Mater, 2024, 31:463-474
S2924 Laduviglusib (CHIR-99021) HCl Laduviglusib (CHIR-99021; CT99021) HCl is hydrochloride of CHIR-99021, which is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs Cdc2 and ERK2. CHIR-99021 is a potent pharmacological activators of the Wnt/beta-catenin signaling pathway. CHIR-99021 significantly rescues light-induced autophagy and augments GR, RORα and autophagy-related proteins.
Nat Cancer, 2024, 10.1038/s43018-023-00716-7
Nat Commun, 2024, 15(1):1285
Nat Commun, 2024, 15(1):668
S8178 BML-284 (Wnt agonist 1) BML-284 (Wnt agonist 1) is a cell permeable Wnt signaling pathway activator, which induces β-catenin- and TCF-dependent transcriptional activity with EC50 of 0.7 μM.
Cell Rep Med, 2023, 4(1):100881
Mol Med, 2023, 29(1):101
Mol Med, 2023, 29(1):101
S7954 CP21R7 CP21R7 is a potent and selective GSK-3β inhibitor that can potently activate canonical Wnt signalling.
Cell, 2022, 185(14):2523-2541.e30
Sci Rep, 2022, 12(1):7
ACS Nano, 2021, 10.1021/acsnano.1c06452
S7421 CGP 57380 CGP 57380 is a potent MNK1 inhibitor with IC50 of 2.2 μM, exhibiting no inhibitory activity on p38, JNK1, ERK1 and -2, PKC, or c-Src-like kinases. CGP 57380 upregulates β-catenin and potentiates radiation-induced apoptosis.
Cell Commun Signal, 2023, 21(1):107
Fundam Clin Pharmacol, 2022, 10.1111/fcp.12759
J Cancer, 2020, 11(4):990-996
S7914 Isoxazole 9 (ISX-9) Isoxazole 9 (Isx-9) is a synthetic promotor of adult neurogenesis by triggering neuronal differentiation of adult neural stem/precursor cells (NSPCs). Isoxazole 9 (Isx-9) activates multiple pathways including TGF-β induced epithelial–mesenchymal transition (EMT) signaling, canonical and non-canonical Wnt signaling at different stages of cardiac differentiation.
Commun Biol, 2022, 5(1):750
Front Cell Dev Biol, 2021, 9:728352
Front Cell Dev Biol, 2021, 9:728352
S3630 Methyl Vanillate Methyl Vanillate, one of the ingredients in Hovenia dulcis Thunb, activates the Wnt/β-catenin pathway and induces osteoblast differentiation in vitro.
Sci Rep, 2022, 12(1):7
S3223 L-Quebrachitol L-Quebrachitol (L-QCT), a natural product isolated from many plants, promotes proliferation and cell DNA synthesis. L-Quebrachitol upregulates bone morphogenetic protein-2 (BMP-2) and runt-related transcription factor-2 (Runx2) and regulatory genes associated with mitogen-activated protein kinase (MAPK) and Wnt/β-catenin signaling pathway, while down-regulating the receptor activator of the nuclear factor-κB(NF-κB) ligand (RANKL) mRNA level.
E0072 Indirubin-3′-oxime Indirubin-3′-oxime (IDR3O, I3O) is an indirubin analogue that shows favorable inhibitory activity targeting GSK-3β and CDKs. Indirubin-3′-oxime also inhibits JNKs with IC50s of 0.8 μM, 1.4 μM, and 1.0 μM for JNK1, JNK2, and JNK3, respectively. Indirubin-3′-oxime activates Wnt/β-catenin signaling and inhibits adipocyte differentiation and obesity.
S6085 KY19382 (A3051) KY19382 (A3051) is a Wnt/β-catenin signalling activator through inhibitory effects on both CXXC5–DVL interaction and GSK3β activity with IC50s of 19 nM and 10 nM, respectively.
S8647 iCRT3 iCRT3 is an antagonist of Wnt/β-catenin signaling with an IC50 of 8.2 nM in the Wnt responsive STF16-luc reporter assays.
EMBO J, 2022, 41(15):e110218
EMBO Mol Med, 2022, e14990
Gastroenterology, 2021, S0016-5085(21)03489-2
S0733 Tegatrabetan (BC-2059) Tegatrabetan (BC2059,Tegavivint) is an antagonist of β-Catenin. Tegatrabetan (BC2059) treatment disrupts the binding of β-catenin with the scaffold protein transducin β-like 1 (TBL1) and proteasomal degradation and declines in the nuclear levels of β-catenin.
S8320 SKL2001 SKL2001 is a novel agonist of the Wnt/β-catenin pathway. It disrupts the Axin/β-catenin interaction.
Nat Cancer, 2024, 10.1038/s43018-023-00716-7
Int J Biol Sci, 2024, 20(3):848-863
Cell Death Dis, 2023, 14(10):696
S5815 WAY-316606 WAY-316606, a specific antagonist of SFRP1, functions as an activator of canonical Wnt/β-catenin signalling in the human hair bulb.
Stem Cells Transl Med, 2024, szae006
J Bone Miner Res, 2021, 10.1002/jbmr.4435
S9828 WAY-262611 WAY-262611 (BML-WN110, Compound 5) is a beta-catenin (β-Catenin) agonist that increases bone formation rate with EC50 of 0.63 μM in TCF-Luciferase assay. WAY-262611 is also an inhibitor of dickkopf 1 (DKK1).
J Orthop Surg Res, 2023, 18(1):751
Nat Commun, 2022, 13(1):7194
S5992 Heparan Sulfate Heparan sulfate (HS, Heparitin sulfate, Alpha-idosane, HHS 5, N-Acetylheparan Sulfate, Suleparoid, Tavidan), a constituent of HS proteoglycans (HSPGs), is a linear polysaccharide present on the cell surface. Heparan sulfate influences the binding affinity of intestinal epithelium cells (IECs) to Wnt, thereby promoting activation of canonical Wnt signaling and facilitating regeneration of small intestinal crypts after epithelial injury.
Mol Genet Genomics, 2022, 297(2):397-405
PeerJ, 2022, 10:e14003
Glycobiology, 2019, 29-8:572-581
S6961 Foxy-5 Foxy-5, a Wnt-5a mimicking hexapeptide, is a WNT signalling pathway modulator potentially for the treatment of metastatic breast cancer, prostate cancer and colorectal cancer.
CNS Neurosci Ther, 2023, 10.1111/cns.14099
S0458 KY1220 KY1220 is a small molecule that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway with IC50 of 2.1 μM in HEK293 reporter cells.
E1731New 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 ApcMin mice.
Commun Biol, 2023, 6(1):197
E1486New Zamaporvint (RXC004) Zamaporvint (RXC004) is an orally active and selective inhibitor of Wnt. It targets membrane-bound o-acyltransferase Porcupine and inhibits Wnt ligand palmitoylation, secretion, and pathway activation. RXC004 exhibits potent antiproliferative effects in Wnt ligand-dependent colorectal and pancreatic cell lines and possesses multiple antitumor mechanisms.

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