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Wnt inhibitor
KY02111 is a potent and selective Wnt signaling pathway inhibitor discovered by a cell-based screening, which promotes differentiation of hESCs/iPSCs to cardiomyocytes when used at the second stage of differenitation.- Abinayaselvi Murugan, .et al. , bioRxiv, 2024, February 22
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PARP inhibitor
XAV 939 is a TNKS inhibitor (IC50 values are 0.011 and 0.004 μM for TNKS1 and TNKS2 respectively).- Esteban Zamudio-Martínez, .et al. , Cell Commun Signal, 2025, Nov 5;23:477 PMID: 41194181
- Shizu Aikawa, .et al. , EMBO J, 2017, Jul 14; 36(14): 2146-2160 PMID: 28588064
- Mikaël M. Martino, .et al. , Nat Commun, 2016, 7: 11051 PMID: 27001940
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Wnt/beta-catenin inhibitor
ICG-001 is a specific inhibitor of Wnt/β-catenin signaling pathway that inhibits β-catenin/cyclic AMP response element-binding (CREB) protein transcription (IC50=3 microM) .- Hong Gao, .et al. , Sci Rep, 2024, Oct 15;14(1):24182 PMID: 39406776
- Yun-Sheng Chen, .et al. , Research Square, 2024, August 16th
- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Seonmin Choi, .et al. , Yonsei Med J, 2021, Nov;62(11):1042-1051 PMID: 34672138
- Jasper C.Munro, .et al. , Livest Sci, 2019, 229 (2019) 159-169
- Kim JH, .et al. , Cell Rep, 2019, May 14;27(7):2105-2118.e5 PMID: 31091449
- Yamaoka R, .et al. , J Surg Oncol, 2018, Sep;118(4):664-674 PMID: 30196535
- Aida Y, .et al. , In Vitro Cell Dev Biol Anim, 2018, Jun;54(6):468-476 PMID: 29785536
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PORCN/Wnt inhibitor
Wnt-C59 is a very potent and highly selective Wnt signaling antagonist with an IC50 ~ 74 pM in the Wnt signaling reporter assay.- Laksitorini MD, .et al. , Sci Rep, 2019, Dec 23;9(1):19718 PMID: 31873116
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Wnt agonist 1
Wnt agonist 1 is a cell-permeable Wnt signaling activator. It nduces beta-catenin and TCF-dependent transcriptional activity with EC50 value of 0.7 uM.- Lingling Chen, .et al. , Biochem Pharmacol, 2024, Nov 29:232:116688 PMID: 39617210
- Abinayaselvi Murugan, .et al. , bioRxiv, 2024, February 22
- Zhao-Hui Chen, .et al. , Breast Cancer Res, 2023, 25: 22 PMID: 36829181
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CBP/beta-catenin antagonist
PRI-724 is the second-generation, potent and specific inhibitor of CBP/β-Catenin complex, and a modulator of the β-Catenin dependent canonical Wnt signaling pathway in cancer stem cells.
- Paul Mark Medina, .et al. , Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
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PORCN inhibitor
LGK974 is a highly potent, selective and orally bioavailable Porcupine inhibitor (Wnt signaling antagonist) with an IC50 <1 nM in the Wnt signaling reporter assay and Porcupine binding assay.- Uxia Gurriaran-Rodriguez, .et al. , Sci Adv, 2024, Dec 13;10(50):eado5914 PMID: 39661666
- Sho Tsukamoto, .et al. , Development, 2023, Aug 1;150(15):dev201734 PMID: 37539462
- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- A-Ri Cho, .et al. , Sci Rep, 2022, Apr 29;12(1):7013 PMID: 35487932
- Yang JM, .et al. , Toxicology, 2018, Dec 1;410:65-72 PMID: 30205152
- E Lemieux, .et al. , Oncogene, 2015, Sep 17; 34(38): 4914-4927 PMID: 25500543
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Wnt inhibitor
JW74 is an efficient and specific inhibitor of the canonical Wnt signaling. JW74 shows a reduction of canonical Wnt signaling in the ST-Luc assay with IC50 values of 790 nM.- Yang JM, .et al. , Toxicology, 2018, Dec 1;410:65-72 PMID: 30205152
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Wnt inhibitor
IWR-1-endo is a potent inhibitor of the Wnt response, blocking a cell-based Wnt/β-catenin pathway reporter response with an IC50 value of 180 nM. Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription.- Yuichi Akaba, .et al. , iScience, 2025, Oct 16;28(11):113789 PMID: 41244585
- Charles A.Herring, .et al. , Cell, 2022, Oct 27;S0092-8674(22)01258-2 PMID: 36318921
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Wnt/β-Catenin Inhibitor
MSAB is a potent and selective Wnt/β-catenin signaling inhibitor. By binding to β-catenin, it promotes its degradation and effectively downregulates Wnt/β-catenin target genes. MSAB demonstrates significant anti-tumor activity, particularly in Wnt-dependent cancer cell lines, making it a valuable tool for cancer research and therapeutic development targeting aberrant Wnt signaling. -
Dishevelled Protein PDZ Domain Inhibitor
3289-8625 is a potent inhibitor of the PDZ domain of Dishevelled (Dvl) protein, exhibiting a Kd of 10.6 μM. This compound effectively inhibits Wnt signaling pathways and demonstrates a significant impact on prostate cancer PC-3 cell growth, with an IC50 of 12.5 μM. 3289-8625 is valuable for research involving embryonic development and cancer biology. -
Neurogenesis Inducer
Neurodazine is a neurogenesis inducer that promotes the differentiation of pluripotent cells into neuronal lineages. This compound activates the Wnt and Shh signaling pathways, facilitating neural development and potentially improving neuroregeneration applications. Neurodazine is suitable for research in developmental biology, neuroscience, and regenerative medicine. -
DKK1 Inhibitor
Gallocyanine chloride is a DKK1 inhibitor that targets the DKK1/LRP6 interaction, exhibiting an IC50 of 6.38 μM. This compound is relevant for research into Alzheimer's disease and related neurodegenerative tauopathies, as it activates the Wnt signaling pathway and promotes β-catenin accumulation. Additionally, Gallocyanine chloride demonstrates anti-metastatic, anti-inflammatory, and anti-fibrotic properties, and can serve as a fluorescent probe for the detection of superoxide anion radicals. -
NLRP3 Activator
Nigericin is an antibiotic derived from Streptomyces hygroscopicus that act as a K+/H+ ionophore, promoting K+/H+ exchange across mitochondrial membranes. Nigericin is a NLRP3 activator. Nigericin shows promising anti-cancer activities through decreasing intracellular pH (pHi), and inactivation of Wnt/β-catenin signals. Nigericin induces pyroptosis through caspase 1/GSDMD in TNBC. -
p53 Activator/Wnt Inhibitor
PAWI-2 is a p53 activator and Wnt inhibitor that targets β3-KRAS signaling independently of KRAS. This compound selectively inhibits the phosphorylation of TBK1, resulting in the activation of apoptotic pathways, evidenced by increased caspase-3/7 activity and PARP cleavage. Additionally, PAWI-2 facilitates the translocation of optineurin into the nucleus and induces G2/M cell cycle arrest. It effectively reverses cancer stemness and overcomes drug resistance in integrin β3 KRAS-dependent human pancreatic cancer stem cells, demonstrating significant tumor growth inhibition in orthotopic xenograft mouse models. -
Wnt inhibitor
Cardionogen 1 (CDNG1/vuc230) is an inhibitor of the Wnt signaling pathway that suppresses Myc-induced liver tumorigenesis. In zebrafish embryos, Cardionogen 1 inhibits cardiomyocyte formation when administered before gastrulation, but promotes cardiomyocyte formation when applied during or after gastrulation. It holds potential for research in cancer and cardiovascular disease. -
TET2 inhibitor
TFMB-(S)-2-HG is a potent inhibitor of TET2 and EglN prolyl hydroxylases. It downregulates Wnt3a and intranuclear β-catenin protein expression, and inhibits osteogenic differentiation of cells. TFMB-(S)-2-HG shows potential for research in acute myeloid leukemia (AML). -
Wnt inhibitor
Zamaporvint (RXC004) is an orally active and selective Wnt pathway inhibitor that targets the membrane-bound O-acyltransferase Porcupine. By inhibiting Wnt ligand palmitoylation, it blocks Wnt ligand secretion and downstream pathway activation. Zamaporvint exhibits a favorable pharmacokinetic profile and shows potent antiproliferative activity in Wnt ligand-dependent colorectal and pancreatic cancer cell lines. With multiple antitumor mechanisms, it is a promising agent for cancer research. - Withanolide B, a bioactive constituent of *Withania somnifera* Dunal, promotes osteogenic differentiation of human bone marrow-derived mesenchymal stem cells (hBMSCs) through activation of the ERK1/2 and Wnt/β-catenin signaling pathways. It also demonstrates neuroprotective, anti-arthritic, anti-aging, and anti-cancer properties.
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β-catenin PROTAC degrader
xStAx-VHLL is a PROTAC degrader targeting β-catenin, promoting its ubiquitination and proteasomal degradation. It effectively inhibits the Wnt/β-catenin signaling pathway and suppresses proliferation of colon cancer cells, demonstrating anti-tumor activity. -
Wnt/β-catenin Inhibitor
CCT036477 is a selective inhibitor of the Wnt/β-catenin signaling pathway that effectively disrupts β-catenin-mediated transcription without affecting its overall levels. This compound demonstrates significant anti-proliferative effects on various cancer cell lines and impairs embryonic development. Additionally, CCT036477 downregulates the expression of key Wnt target genes, including PPARδ, Cyclin D1, TCF4, and ID2, making it a valuable tool for research in cancer biology and developmental studies. -
Wnt/β-catenin/NF-κB/AP-1 Inhibitor
Chikusetsusaponin IVa methyl ester is a natural triterpenoid saponin that functions as a Wnt/β-catenin, NF-κB, and AP-1 inhibitor. It induces G0/G1 cell cycle arrest and apoptosis in colon cancer cells through the inhibition of the Wnt/β-catenin signaling pathway. Additionally, this compound significantly decreases the production of nitric oxide, prostaglandin E₂, and pro-inflammatory cytokines, while downregulating iNOS and COX-2 levels. Chikusetsusaponin IVa methyl ester is valuable for research focused on colorectal cancer and inflammatory processes. -
Wnt/β-catenin Inhibitor
Windorphen is a selective Wnt/β-catenin signaling inhibitor that specifically interferes with the c-terminal transactivation domain of β-catenin-1, while leaving β-catenin-2 unaffected. This compound targets p300, effectively disrupting the interaction between β-catenin and p300 without impacting CBP. Windorphen is valuable for research applications focused on β-catenin-related pathways, cancer biology, and developmental processes. -
WNT7A Inhibitor/Photosensitizer
WNT7A-IN-1 sodium is a selective inhibitor of WNT7A that disrupts the interaction between WNT7A and its receptor FZD5, leading to enhanced expression of MHC-I. This reagent is known to significantly increase levels of MHC-I and phosphorylated p65 while decreasing active β-catenin expression. Additionally, WNT7A-IN-1 sodium acts as a photosensitizer in the green spectral region, making it suitable for applications in photodynamic therapy and immunological studies. -
Wnt Agonist
Wnt/β-catenin agonist 4 (Derivative 83) is a potent agonist of the Wnt signaling pathway that stimulates Wnt/β-catenin signal transmission. This compound plays a crucial role in enhancing cellular processes regulated by Wnt signaling, such as cell proliferation, differentiation, and tissue regeneration. It is useful in various research applications, including studies on developmental biology, cancer progression, and regenerative medicine. -
Wnt Activator
Dalosirvat is a potent Wnt activator that effectively enhances Wnt signaling pathways. With an EC50 of 28-29 nM, it demonstrates significant biological activity in promoting cell proliferation and differentiation in various contexts. This compound is primarily utilized in research applications related to developmental biology, cancer research, and regenerative medicine, facilitating investigations into the roles of Wnt signaling in cellular processes. -
Wnt Inhibitor
Wnt Pathway Inhibitor 3 is a potent inhibitor of the Wnt signaling pathway, exhibiting an IC50 value of 45 nM. This compound demonstrates significant antiproliferative activity, making it a valuable tool for research in cancer biology and developmental studies. Its ability to modulate Wnt signaling can aid in the exploration of various cellular processes and disease mechanisms. -
Wnt Signaling Inhibitor
JW67 is a potent Wnt signaling inhibitor that targets the multiprotein complex composed of β-catenin, GSK-3β, AXIN, APC, and CK1, demonstrating an IC50 of 1.17 µM. By effectively reducing active β-catenin levels, JW67 leads to the downregulation of Wnt target genes, making it a valuable tool for studying Wnt signaling pathways. Additionally, JW67 inhibits the growth of colorectal cancer cells, providing potential applications in cancer research and therapeutic development. -
Wnt Activator
Wnt Pathway Activator 2 is a potent activator of the Wnt signaling pathway, exhibiting an EC50 value of 13 nM. This compound promotes Wnt pathway activation, making it a valuable tool for researching developmental biology and cancer progression. Its ability to modulate Wnt signaling can facilitate studies on cellular processes such as proliferation, differentiation, and stem cell biology. -
Wnt Inhibitor
Ipafricept is a recombinant fusion protein that functions as a Wnt inhibitor by binding to Wnt ligands via the extracellular portion of the human Frizzled-8 receptor fused with a human IgG1 Fc fragment. This mechanism effectively blocks Wnt signaling pathways, leading to reduced tumor growth and decreased liver and lung metastases when combined with Gemcitabine in pancreatic cancer mouse models. Additionally, Ipafricept demonstrates significant inhibitory activity against solid tumors, including desmoid tumor, germ cell cancer, and ovarian cancer, with an acceptable tolerance profile. -
Wnt Signaling Inhibitor
Coronaridine is an iboga alkaloid that functions as a Wnt signaling pathway inhibitor, effectively reducing β-catenin expression. This compound is primarily employed in research related to cancer biology, stem cell differentiation, and developmental processes, where dysregulation of the Wnt pathway is implicated. Its ability to modulate β-catenin levels makes it a valuable tool for investigating the mechanistic roles of Wnt signaling in various biological contexts. -
Wnt Inhibitor
WIC1 is a potent Wnt signaling inhibitor that targets the Wnt pathway, crucial for various biological processes, including cell proliferation and differentiation. This compound demonstrates significant anti-cancer activity by disrupting Wnt-mediated transcriptional activation, making it valuable for cancer research. WIC1 can be utilized in investigations of tumor growth, metastasis, and the overall role of Wnt signaling in oncogenesis. -
Wnt Inhibitor
Gigantol isomer-1 is a bibenzyl compound that functions as a Wnt inhibitor. This compound demonstrates significant therapeutic potential by targeting cancer cell proliferation and survival through modulation of the Wnt/β-catenin signaling pathway. Its capability to disrupt this crucial pathway makes it a valuable tool for research applications focused on cancer biology and therapeutic development. -
WNT1 Inhibitor
SJ26 is a potent Wnt1 inhibitor that exhibits anticancer activity. By targeting and inhibiting the expression of Wnt1, SJ26 disrupts Wnt1-mediated downstream signaling pathways, leading to a reduction in the migratory capacity of cancer cells. This compound is valuable for research focused on cancer progression and the role of Wnt signaling in tumor metastasis. -
Wnt/β-catenin Inhibitor
15-Oxospiramilactone is a diterpene derivative that functions as a Wnt/β-catenin signaling inhibitor. It exhibits significant biological activity by suppressing tumorigenesis in colon cancer cells, making it a valuable reagent for cancer research. This compound is suitable for studies investigating the modulation of the Wnt pathway and its implications in colorectal cancer progression. -
WNT7A Inhibitor/Photosensitizer
WNT7A-IN-1 is a WNT7A inhibitor that disrupts the interaction between WNT7A and its receptor FZD5, leading to the upregulation of MHC-I expression. This compound enhances the expression of MHC-I and phosphorylated p65 while decreasing the levels of active β-catenin. Additionally, WNT7A-IN-1 serves as a photosensitizer in the green spectral region, making it valuable for research in cancer immunotherapy and photodynamic therapy applications. -
Wnt Pathway Inhibitor
Wnt Pathway Inhibitor 5 is a potent inhibitor of the Wnt signaling pathway, exhibiting an IC50 value of less than 0.003 µM. This compound demonstrates significant anti-cancer activity, making it effective against various malignancies such as ovarian teratocarcinoma, breast cancer, osteosarcoma, and head and neck squamous carcinoma. It serves as a valuable tool for researchers investigating the role of Wnt signaling in cancer progression and therapeutic interventions. -
Wnt Activator
XD23 is a potent Wnt activator that functions by downregulating DKK1, thereby enhancing the WNT/β-catenin signaling pathway. This compound demonstrates significant biological activity in osteosarcoma inhibition, making it a valuable tool for research into bone cancer and related signaling mechanisms. Its ability to modulate Wnt signaling opens avenues for investigating therapeutic strategies targeting Wnt-related pathways in various cancers. -
Wnt/β-catenin Pathway Inhibitor
IWP-2-V2 is an analogue of IWP-2 that effectively inhibits the Wnt/β-catenin signaling pathway. This compound plays a significant role in modulating cellular processes related to development and cancer, making it a valuable tool for researchers studying the implications of Wnt signaling in various biological contexts. Its ability to disrupt β-catenin-mediated transcriptional activity positions IWP-2-V2 as a potential candidate for investigations into regenerative medicine and cancer therapy. -
Wnt Signaling Activator
BML-284 hydrochloride is a potent Wnt signaling activator that enhances TCF-dependent transcriptional activity. It demonstrates an effective EC50 of 700 nM, making it suitable for researching Wnt pathway modulation. This compound is valuable for studies related to developmental biology, cancer research, and other fields that investigate the role of Wnt signaling in cellular processes. -
Wnt Pathway Inhibitor
SEN461 is a potent and orally bioavailable inhibitor of the Wnt signaling pathway. This compound demonstrates significant anti-tumor activity, making it a valuable tool for research applications in glioblastoma multiforme (GBM) and other cancers driven by aberrant Wnt pathway activation. Its efficacy in modulating Wnt-related processes highlights its potential for therapeutic development and mechanistic studies in cancer biology. -
Wnt/b-catenin Inhibitor
21H7 is a selective inhibitor of the Wnt/β-catenin signaling pathway. This compound significantly inhibits cell proliferation in hair follicles and demonstrates potent growth suppression of breast and colon cancer cells. Due to its specific targeting of the Wnt/β-catenin pathway, 21H7 serves as a valuable tool in cancer research and therapeutic development. -
Wnt Signal Inhibitor
Wnt/β-catenin-IN-7 is a Wnt signaling pathway inhibitor with an IC50 of 0.15 μM. This compound effectively disrupts β-catenin-mediated transcriptional activation, making it valuable for investigating the role of Wnt signaling in cancer and fibrosis. Its potent inhibitory activity supports research into therapeutic targets within these pathological conditions. -
Wnt/β-catenin Inhibitor
Wnt/β-catenin-IN-4 is a potent inhibitor of the Wnt/β-catenin signaling pathway. This compound effectively disrupts β-catenin-dependent transcription, making it a valuable tool for investigating the role of Wnt signaling in various biological processes. It is commonly utilized in cancer research, developmental biology, and studies related to stem cell differentiation. -
WNT5A Antagonist
MDGCEL is a WNT5A peptide that functions as an antagonist to WNT5A signaling. It mimics WNT5A, providing utility in research focused on modulating WNT signaling pathways. MDGCEL is valuable in studies investigating developmental biology, cell signaling, and cancer research, where the regulation of WNT5A activity is crucial. -
Wnt5a Antagonist
Box5 is a potent antagonist of Wnt5a, specifically designed to inhibit Wnt5a signaling pathways. This compound effectively reduces Wnt5a-mediated calcium ion release and inhibits cell migration, making it a valuable tool in the study of cellular dynamics. Box5 has significant potential for research applications in melanoma, facilitating the exploration of therapeutic interventions targeting Wnt5a signaling. -
WNT5A Agonist
Foxy-5 is a WNT5A agonist that functions as a mimetic peptide of the WNT5A protein, a key player in non-canonical Wnt signaling pathways. It induces cytosolic free calcium signaling while leaving β-catenin activation unaffected, and has been shown to inhibit the migration and invasion of epithelial cancer cells. Additionally, Foxy-5 effectively reduces metastatic spread in WNT5A-low prostate cancer cells within an orthotopic mouse model, making it a valuable reagent for cancer research and therapeutic investigations. -
Wnt inhibitor
IWP-3 is an inhibitor of Wnt production. Blocks Wnt pathway activity in vitro ( IC?????€ = 40 nM). IWP-3 inactivates Porcupine (Porcn), a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion. Through blockade of Wnt signaling, IWP-3 has been used to promote cardiomyocyte generation from human embryonic stem cells (EC?????€ = 1.2 μM).

