Wnt/beta-catenin

Inhibitory Selectivity

Isoform-specific Inhibitors

Wnt/beta-catenin Products

All (36) Wnt/beta-catenin Inhibitors (23) Wnt/beta-catenin Activators (6) Wnt/beta-catenin Antagonists (2) Wnt/beta-catenin Agonists (3) Wnt/beta-catenin Modulators (2) New Wnt/beta-catenin Products

Catalog No.	Information	Product Use Citations	Product Validations
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.	Cell, 2021, 184(12):3299-3317.e22 Sci Adv, 2021, 7(33)eabf4416 Nat Commun, 2021, 12(1):4090	Fluorescence microscopy of pSuper or Cdo shRNA expressing P19 cells at ITS1 immunostained withβ-tubulin III antibodies. Size bar=100 um. P19/control or P19/Cdo shRNA cells were treated with DMSO or XAV939 in the differentiation medium for 72 h followed by immunostaining.
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.	Nat Cell Biol, 2021, 23(3):257-267 Bioact Mater, 2021, 6(10):3343-3357 Redox Biol, 2021, 39:101811	ICG-001 variably influences Wnt transcriptional activity across pancreatic cancer lines. Nuclear extracts from AsPC-1 cells treated with vehicle or 30 umol/L ICG-001 for 6 hours were immunoprecipitated with anti-CBP or control IgG antibodies followed by Western blot analyses for β-catenin and CBP.
S7086	IWR-1-endo IWR-1-endo (endo-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, 2021, 12(1):4535 Proc Natl Acad Sci U S A, 2021, 118(15)e2018505118 Redox Biol, 2021, 39:101811	Effect of IWR-1 treatment on total β-catenin levels and adipogenesis in high-passage shSCR and shTCF7L2 cells. Cells were treated with IWR-1 (10 μmol/L) every other day for 6 days during differentiation. Western blot demonstrates the effect of IWR-1 on total β-catenin protein levels at the end of adipogenesis (each lane represents a single independent adipogenesis experiment, n = 4 for each treatment).
S7096	KY02111 KY02111 promotes differentiation of hPSCs to cardiomyocytes by inhibiting Wnt signaling, may act downstream of APC and GSK3β.	Stem Cells, 2021, 10.1002/stem.3328 J Biosci Bioeng, 2021, S1389-1723(21)00114-6 Carcinogenesis, 2020, 41(7):993-1004	Transient Wnt inhibition results in persistent decrease of b-catenin. HTM cells were incubated for 4 days in serum-free media, treated with Wnt inhibitors for 8 days in serum free media, and recovered for 4 days in serum-free media before being fixed and stained for b-catenin. (B) HTM cells treated with 10 μM KY02111 or LGK-974 likewise show a reduction of b-catenin staining intensity. (CeD) Quantification of b-catenin staining intensity in HTM cells from 3 donors indicates a statistically significant decrease in intensity after 0.5 μg/mL SFRP1 (SFRP1), 10 μM KY02111, and 10 μM LGK-974. (E) Western blot shows increased T41 phosphorylation of b-catenin after SFRP1 or KY02111 treatment. Data presented as mean ± SEM. Significant difference from control using Tukey's method denoted by * p < 0.05; ***p < 0.001; using Student's T-test denoted by #p < 0.05. n=3. Scale bar 50 μm.
E0033^New	IWP-4 IWP-4 is a potent Wnt/β-catenin signaling pathway inhibitor with an IC50 of 25 nM.
S5992^New	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.
S6085^New	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.
S6961^New	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.
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, 2021, 12(1):2551 Front Cell Dev Biol, 2021, 9:644667 Stem Cell Res Ther, 2021, 12(1):208	KIF3A knockdown promotes both ligand secretion and intracellular signalling of the Wnt/β-catenin pathway in NSCLC cell lines. (c,d) SuperTOPFlash reporter assay to examine the effect of KIF3A knockdown on signalling pathway activation by autocrine or exogenous WNTs in A549 and SW900 cell lines. A549 and SW900 cells were incubated with DMSO or IWP-2 (30 μ M) for 48 h, and then treated with BSA or WNT3A (100 ng/ml) for additional 24 h. Luciferase reporter activity was calculated by dividing TOP/RL ratio by FOP/RL ratio (n = 3; error bars indicate SEM; p-value was determined by one-way ANOVA). P < 0.05; *P < 0.01.
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.
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.
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.	Front Cell Dev Biol, 2020, 8:408
S8429	PNU-74654 PNU-75654 disrupts the Wnt signaling pathway via inhibition of the interaction (KD50=450 nM) between β-catenin and Tcf4.	Cancer Cell, 2021, 39(4):529-547.e7 Mol Cell Endocrinol, 2021, 528:111243 Commun Biol, 2021, 4(1):357
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.	Neoplasia, 2019, 21(4):389-400 J Biol Chem, 2018, 293(52):20014-20028
S7484	FH535 FH535 is a Wnt/β-catenin signaling inhibitor and also a dual PPARγ and PPARδ antagonist.	J Exp Clin Cancer Res, 2021, 40(1):230 Cell Oncol (Dordr), 2021, 10.1007/s13402-021-00590-4 Carcinogenesis, 2020, 41(7):993-1004	Ki-67 staining in xenograft tissues from FH535-treated and control group. Magnifications: ×200 in left column, ×400 in right column.
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.	Cancers (Basel), 2020, 12(10)E3003 FASEB J, 2020, 2 Nat Cell Biol, 2019, 21(5):627-639
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.	Cell Death Dis, 2021, 12(4):316 Int J Mol Sci, 2021, 22(8)4263 Mol Carcinog, 2021, 10.1002/mc.23308
S7490	WIKI4 WIKI4 is a novel Tankyrase inhibitor with IC50 of 15 nM for TNKS2, and leads to inhibition of Wnt/beta-catenin signaling.	Carcinogenesis, 2020, 41(7):993-1004 Nat Commun, 2019, 10(1):4363
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.	Front Cell Dev Biol, 2021, 9:648201
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.	Neoplasia, 2020, 23(1):1-11 Cell Mol Life Sci, 2019, 76(14):2817-2832 Front Genet, 2018, 9:746
S8327	KYA1797K KYA1797K is a highly potent and selective Wnt/β-catenin inhibitor with IC50 of 0.75 µM (TOPflash assay).	Front Endocrinol (Lausanne), 2021, 12:676403 Cell Div, 2020, 1;15:2 J Cell Biochem, 2020, 121(2):1250-1259	A549 cells were treated with KYA1797K for 72 h, cells lysates were collected for western blotting, concentration gradient (1, 12.5 μM, 25 μM) was set for the analysis
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).	Chin J Integr Med, 2021, 10.1007/s11655-021-3282-0 Oncotarget, 2021, 12(7):674-685
S8704	iCRT14 iCRT14 is a β-catenin/Tcf inhibitor with a Ki value of 54 ± 5.2 μM in homogeneous fluorescence polarization (FP) assay.	Theranostics, 2021, 11(6):2966-2986
S2924	CHIR-99021 (CT99021) HCl 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 Genet, 2021, 53(4):467-476 Eur Heart J, 2021, ehab547 Nat Cell Biol, 2021, 23(7):745-757	Inhibition of GSK3 activity induces an autophagic response in human pancreatic cancer cells. PANC1 cells were treated for 24 h with DMSO, CHIR99021 (CHIR; 5 uM) or the mTOR inhibitor Torin1 (250 nM). Autophagosome (punctate LC3B) (D) and lysosome (E) labeling was visualized with a Zeiss LSM700 confocal microscope. Images were acquired with a 20x (D) or 63x (E) objective. Nuclei were stained with DAPI. Scale bars, 20 祄.
S1263	CHIR-99021 (CT99021) 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.	Cell, 2021, 184(11):2843-2859.e20 Nat Genet, 2021, 53(4):467-476 Cancer Cell, 2021, 39(3):407-422.e13	For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of CHIR-99021 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 mM HCl and 0.1% Nonidet-40) was added to dissolve the formazan. The absorbance of each well was measured by ELx808 (BioTek, Winooski, VT) or Wallac Victor2 (Perkin-Elmer Life Sciences, Boston, MA) Microplate Reader. Viable cells are presented as percent of control, vehicle-treated cells.
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.
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.
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.	J Cancer, 2020, 11(4):990-996 Bioorg Med Chem, 2018, 26(16):4602-4614 Cancer Lett, 2016, 10.1016/j.canlet.2016.02.052	PC-3 cells were seeded in 6-well plates. On the next day, cells were treated with the indicated concentrations of 3-AWA, LY294002, CGP57380 or Rapamycin alone and or combination for 12 h. The cells were then subjected to preparation of whole-cell lysates for detection of the indicated proteins using western blotting. The western blots are the representative of three similar experiments.
S8178	Wnt agonist 1 Wnt agonist 1 (BML-284 HCL, AMBMP HCL) is a cell permeable Wnt signaling pathway activator, which induces β-catenin- and TCF-dependent transcriptional activity with EC50 of 0.7 μM.	Cell, 2021, 184(1):243-256.e18 Front Cell Dev Biol, 2021, 9:648201 J Exp Clin Cancer Res, 2021, 40(1):54	Both Wnt sinaling activators of agonist and recombinant protein, and therapeutic agents of fluorouracil and docetaxel stimulated TCF-4 promoter functions of wild-type (wt) could be blocked by Nano-Let-7b, compared with negative control group of mutant-type (mut). In detail, Let-7b alone affected the TCF-4 promoter activity effectively, and wnt signaling activators of either Wnt agonist-1 or Wnt protein attenuated the Let-7b functions significantly. Combined usage of therapeutic agent of either fluorouracil or docetaxel with Let-7b increased the TCF-4 activity when compared to groups treated with Let-7b alone, however, the TCF-4 activity when applying combination was still significantly lower than that of controlled group
S0733	Tegatrabetan (BC-2059) Tegatrabetan (BC2059) 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.
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.	Cancer Manag Res, 2021, 13:1901-1907 Biochem Biophys Res Commun, 2021, 552:66-72 J Clin Invest, 2020, 130(8):4301-4319
S9828^New	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).
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.
S8320	SKL2001 SKL2001 is a novel agonist of the Wnt/β-catenin pathway. It disrupts the Axin/β-catenin interaction.	Antioxid Redox Signal, 2021, 10.1089/ars.2020.8200 Cell Death Discov, 2021, 7(1):109 Cancer Cell Int, 2021, 21(1):360	Western blots of nuclear and cytoplasmic fractions of β-catenin and total CDH3. d The ratio of nuclear/cytosolic of β-catenin was calculated by densitometry analysis.
S2431	TMTD (Tetramethylthiuram disulfide) TMTD (Tetramethylthiuram disulfide) can reduce the growth performance of chickens through decreasing liver index, whereas increasing kidney, cardiac, and spleen index, and induces tibial dyschondrolplasia (TD) by changing the expressions of VEGF, HIF-1α and WNT4. TMTD (Tetramethylthiuram disulfide) is widely used in rubber processing as an ultra accelerator for low-temperature cures and in agriculture as an important pesticide.
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.

Catalog No.	Information	Product Use Citations	Product Validations
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.	Cell, 2021, 184(12):3299-3317.e22 Sci Adv, 2021, 7(33)eabf4416 Nat Commun, 2021, 12(1):4090	Fluorescence microscopy of pSuper or Cdo shRNA expressing P19 cells at ITS1 immunostained withβ-tubulin III antibodies. Size bar=100 um. P19/control or P19/Cdo shRNA cells were treated with DMSO or XAV939 in the differentiation medium for 72 h followed by immunostaining.
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.	Nat Cell Biol, 2021, 23(3):257-267 Bioact Mater, 2021, 6(10):3343-3357 Redox Biol, 2021, 39:101811	ICG-001 variably influences Wnt transcriptional activity across pancreatic cancer lines. Nuclear extracts from AsPC-1 cells treated with vehicle or 30 umol/L ICG-001 for 6 hours were immunoprecipitated with anti-CBP or control IgG antibodies followed by Western blot analyses for β-catenin and CBP.
S7086	IWR-1-endo IWR-1-endo (endo-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, 2021, 12(1):4535 Proc Natl Acad Sci U S A, 2021, 118(15)e2018505118 Redox Biol, 2021, 39:101811	Effect of IWR-1 treatment on total β-catenin levels and adipogenesis in high-passage shSCR and shTCF7L2 cells. Cells were treated with IWR-1 (10 μmol/L) every other day for 6 days during differentiation. Western blot demonstrates the effect of IWR-1 on total β-catenin protein levels at the end of adipogenesis (each lane represents a single independent adipogenesis experiment, n = 4 for each treatment).
S7096	KY02111 KY02111 promotes differentiation of hPSCs to cardiomyocytes by inhibiting Wnt signaling, may act downstream of APC and GSK3β.	Stem Cells, 2021, 10.1002/stem.3328 J Biosci Bioeng, 2021, S1389-1723(21)00114-6 Carcinogenesis, 2020, 41(7):993-1004	Transient Wnt inhibition results in persistent decrease of b-catenin. HTM cells were incubated for 4 days in serum-free media, treated with Wnt inhibitors for 8 days in serum free media, and recovered for 4 days in serum-free media before being fixed and stained for b-catenin. (B) HTM cells treated with 10 μM KY02111 or LGK-974 likewise show a reduction of b-catenin staining intensity. (CeD) Quantification of b-catenin staining intensity in HTM cells from 3 donors indicates a statistically significant decrease in intensity after 0.5 μg/mL SFRP1 (SFRP1), 10 μM KY02111, and 10 μM LGK-974. (E) Western blot shows increased T41 phosphorylation of b-catenin after SFRP1 or KY02111 treatment. Data presented as mean ± SEM. Significant difference from control using Tukey's method denoted by * p < 0.05; ***p < 0.001; using Student's T-test denoted by #p < 0.05. n=3. Scale bar 50 μm.
E0033^New	IWP-4 IWP-4 is a potent Wnt/β-catenin signaling pathway inhibitor with an IC50 of 25 nM.
S5992^New	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.
S6085^New	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.
S6961^New	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.
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, 2021, 12(1):2551 Front Cell Dev Biol, 2021, 9:644667 Stem Cell Res Ther, 2021, 12(1):208	KIF3A knockdown promotes both ligand secretion and intracellular signalling of the Wnt/β-catenin pathway in NSCLC cell lines. (c,d) SuperTOPFlash reporter assay to examine the effect of KIF3A knockdown on signalling pathway activation by autocrine or exogenous WNTs in A549 and SW900 cell lines. A549 and SW900 cells were incubated with DMSO or IWP-2 (30 μ M) for 48 h, and then treated with BSA or WNT3A (100 ng/ml) for additional 24 h. Luciferase reporter activity was calculated by dividing TOP/RL ratio by FOP/RL ratio (n = 3; error bars indicate SEM; p-value was determined by one-way ANOVA). P < 0.05; *P < 0.01.
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.
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.
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.	Front Cell Dev Biol, 2020, 8:408
S8429	PNU-74654 PNU-75654 disrupts the Wnt signaling pathway via inhibition of the interaction (KD50=450 nM) between β-catenin and Tcf4.	Cancer Cell, 2021, 39(4):529-547.e7 Mol Cell Endocrinol, 2021, 528:111243 Commun Biol, 2021, 4(1):357
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.	Neoplasia, 2019, 21(4):389-400 J Biol Chem, 2018, 293(52):20014-20028
S7484	FH535 FH535 is a Wnt/β-catenin signaling inhibitor and also a dual PPARγ and PPARδ antagonist.	J Exp Clin Cancer Res, 2021, 40(1):230 Cell Oncol (Dordr), 2021, 10.1007/s13402-021-00590-4 Carcinogenesis, 2020, 41(7):993-1004	Ki-67 staining in xenograft tissues from FH535-treated and control group. Magnifications: ×200 in left column, ×400 in right column.
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.	Cancers (Basel), 2020, 12(10)E3003 FASEB J, 2020, 2 Nat Cell Biol, 2019, 21(5):627-639
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.	Cell Death Dis, 2021, 12(4):316 Int J Mol Sci, 2021, 22(8)4263 Mol Carcinog, 2021, 10.1002/mc.23308
S7490	WIKI4 WIKI4 is a novel Tankyrase inhibitor with IC50 of 15 nM for TNKS2, and leads to inhibition of Wnt/beta-catenin signaling.	Carcinogenesis, 2020, 41(7):993-1004 Nat Commun, 2019, 10(1):4363
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.	Front Cell Dev Biol, 2021, 9:648201
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.	Neoplasia, 2020, 23(1):1-11 Cell Mol Life Sci, 2019, 76(14):2817-2832 Front Genet, 2018, 9:746
S8327	KYA1797K KYA1797K is a highly potent and selective Wnt/β-catenin inhibitor with IC50 of 0.75 µM (TOPflash assay).	Front Endocrinol (Lausanne), 2021, 12:676403 Cell Div, 2020, 1;15:2 J Cell Biochem, 2020, 121(2):1250-1259	A549 cells were treated with KYA1797K for 72 h, cells lysates were collected for western blotting, concentration gradient (1, 12.5 μM, 25 μM) was set for the analysis
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).	Chin J Integr Med, 2021, 10.1007/s11655-021-3282-0 Oncotarget, 2021, 12(7):674-685
S8704	iCRT14 iCRT14 is a β-catenin/Tcf inhibitor with a Ki value of 54 ± 5.2 μM in homogeneous fluorescence polarization (FP) assay.	Theranostics, 2021, 11(6):2966-2986

Catalog No.	Information	Product Use Citations	Product Validations
S2924	CHIR-99021 (CT99021) HCl 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 Genet, 2021, 53(4):467-476 Eur Heart J, 2021, ehab547 Nat Cell Biol, 2021, 23(7):745-757	Inhibition of GSK3 activity induces an autophagic response in human pancreatic cancer cells. PANC1 cells were treated for 24 h with DMSO, CHIR99021 (CHIR; 5 uM) or the mTOR inhibitor Torin1 (250 nM). Autophagosome (punctate LC3B) (D) and lysosome (E) labeling was visualized with a Zeiss LSM700 confocal microscope. Images were acquired with a 20x (D) or 63x (E) objective. Nuclei were stained with DAPI. Scale bars, 20 祄.
S1263	CHIR-99021 (CT99021) 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.	Cell, 2021, 184(11):2843-2859.e20 Nat Genet, 2021, 53(4):467-476 Cancer Cell, 2021, 39(3):407-422.e13	For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of CHIR-99021 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 mM HCl and 0.1% Nonidet-40) was added to dissolve the formazan. The absorbance of each well was measured by ELx808 (BioTek, Winooski, VT) or Wallac Victor2 (Perkin-Elmer Life Sciences, Boston, MA) Microplate Reader. Viable cells are presented as percent of control, vehicle-treated cells.
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.
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.
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.	J Cancer, 2020, 11(4):990-996 Bioorg Med Chem, 2018, 26(16):4602-4614 Cancer Lett, 2016, 10.1016/j.canlet.2016.02.052	PC-3 cells were seeded in 6-well plates. On the next day, cells were treated with the indicated concentrations of 3-AWA, LY294002, CGP57380 or Rapamycin alone and or combination for 12 h. The cells were then subjected to preparation of whole-cell lysates for detection of the indicated proteins using western blotting. The western blots are the representative of three similar experiments.
S8178	Wnt agonist 1 Wnt agonist 1 (BML-284 HCL, AMBMP HCL) is a cell permeable Wnt signaling pathway activator, which induces β-catenin- and TCF-dependent transcriptional activity with EC50 of 0.7 μM.	Cell, 2021, 184(1):243-256.e18 Front Cell Dev Biol, 2021, 9:648201 J Exp Clin Cancer Res, 2021, 40(1):54	Both Wnt sinaling activators of agonist and recombinant protein, and therapeutic agents of fluorouracil and docetaxel stimulated TCF-4 promoter functions of wild-type (wt) could be blocked by Nano-Let-7b, compared with negative control group of mutant-type (mut). In detail, Let-7b alone affected the TCF-4 promoter activity effectively, and wnt signaling activators of either Wnt agonist-1 or Wnt protein attenuated the Let-7b functions significantly. Combined usage of therapeutic agent of either fluorouracil or docetaxel with Let-7b increased the TCF-4 activity when compared to groups treated with Let-7b alone, however, the TCF-4 activity when applying combination was still significantly lower than that of controlled group

Catalog No.	Information	Product Use Citations	Product Validations
S0733	Tegatrabetan (BC-2059) Tegatrabetan (BC2059) 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.
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.	Cancer Manag Res, 2021, 13:1901-1907 Biochem Biophys Res Commun, 2021, 552:66-72 J Clin Invest, 2020, 130(8):4301-4319

Catalog No.

Information

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Product Validations

S0733

Tegatrabetan (BC-2059)

Tegatrabetan (BC2059) 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.

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.

Cancer Manag Res, 2021, 13:1901-1907

Biochem Biophys Res Commun, 2021, 552:66-72

J Clin Invest, 2020, 130(8):4301-4319

Catalog No.	Information	Product Use Citations	Product Validations
S9828^New	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).
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.
S8320	SKL2001 SKL2001 is a novel agonist of the Wnt/β-catenin pathway. It disrupts the Axin/β-catenin interaction.	Antioxid Redox Signal, 2021, 10.1089/ars.2020.8200 Cell Death Discov, 2021, 7(1):109 Cancer Cell Int, 2021, 21(1):360	Western blots of nuclear and cytoplasmic fractions of β-catenin and total CDH3. d The ratio of nuclear/cytosolic of β-catenin was calculated by densitometry analysis.

Catalog No.

Information

Product Use Citations

Product Validations

S9828^New

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).

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.

S8320

SKL2001

SKL2001 is a novel agonist of the Wnt/β-catenin pathway. It disrupts the Axin/β-catenin interaction.

Antioxid Redox Signal, 2021, 10.1089/ars.2020.8200

Cell Death Discov, 2021, 7(1):109

Cancer Cell Int, 2021, 21(1):360

Catalog No.	Information	Product Use Citations	Product Validations
S2431	TMTD (Tetramethylthiuram disulfide) TMTD (Tetramethylthiuram disulfide) can reduce the growth performance of chickens through decreasing liver index, whereas increasing kidney, cardiac, and spleen index, and induces tibial dyschondrolplasia (TD) by changing the expressions of VEGF, HIF-1α and WNT4. TMTD (Tetramethylthiuram disulfide) is widely used in rubber processing as an ultra accelerator for low-temperature cures and in agriculture as an important pesticide.
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.

Catalog No.

Information

Product Use Citations

Product Validations

S2431

TMTD (Tetramethylthiuram disulfide)

TMTD (Tetramethylthiuram disulfide) can reduce the growth performance of chickens through decreasing liver index, whereas increasing kidney, cardiac, and spleen index, and induces tibial dyschondrolplasia (TD) by changing the expressions of VEGF, HIF-1α and WNT4. TMTD (Tetramethylthiuram disulfide) is widely used in rubber processing as an ultra accelerator for low-temperature cures and in agriculture as an important pesticide.

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.

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