-
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
-
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.- Charles A.Herring, .et al. , Cell, 2022, Oct 27;S0092-8674(22)01258-2 PMID: 36318921
- Prodigiosin (Prodigiosine) is a secondary metabolite of Symbiotic bacteria, with anti-fungal and anti-cancer activity.
-
β-Catenin/Tcf Inhibitor
FH535 is an inhibitor of Wnt/β-catenin and PPAR, with anti-tumor activities.- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
-
sFRP-1 inhibitor
WAY-316606 is a small molecule inhibitors of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. -
beta-catenin inhibitor
BC2059 is an orally bioavailable and potent beta-catenin inhibitor.- Ji-Hye Jung, .et al. , Stem Cells Dev, 2016, Jul 1; 25(13): 1006-1019 PMID: 27188501
-
Cardiogenol C is a potent and cell permeable inducer of embryonic stem cell differentiation in cardiomyocytes displaying an Ec50 of 100nm.
-
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
- Cardiogenol C is a diaminopyrimidine compound that induces the differentiation of MHC- (myosin heavy chain) positive cardiomyocytes from embryonic stem cells with an EC50 value of 0.1 uM. Cardiogenol C upregulates cardiac markers and induces cardiac functional properties in lineage-committed progenitor cells.
-
Wnt/beta-catenin inhibitor
Hexachlorophene is a potent KCNQ1/KCNE1 potassium channel activator with EC50 of 4.61 ?? 1.29 uM; also is an inhibitor of Wnt/beta-catenin signaling. -
Bcl-2 Family activator
(E)-Ferulic acid is a isomer of Ferulic acid which is an aromatic compound, abundant in plant cell walls. (E)-Ferulic acid shows a potent ability to remove reactive oxygen species (ROS) and inhibits lipid peroxidation. (E)-Ferulic acid exerts both anti-proliferation and anti-migration effects in the human lung cancer cell line H1299. -
Wnt/β-catenin agonist
Wnt/β-catenin agonist 1 is a Wnt/β-catenin signalling pathway agonist, with an EC50 of 0.27 μM. -
FZD4 agonist
FzM1.8 is an allosteric agonist of the Frizzled receptor FZD4 with pEC50 of 6.4. FzM1.8 binds to FZD4 and activates the WNT/β-catenin pathway, by promoting TCF/LEF transcriptional activity in the absence of any WNT ligand. FzM1.8 binding stabilizes FZD4 with an increased affinity for heterotrimeric G protein and stimulates the release of the Gβγ subunit that in turn activates PI3K. -
Wnt/β-catenin activator
Methyl vanillate, one of the ingredients in Hovenia dulcis Thunb, is a Wnt/β-catenin pathway activator. A benzoate ester that is the methyl ester of vanillic acid. It has a role as an antioxidant and a plant metabolite. - Prodigiosin (Prodigiosine) HCl is a potent proapoptotic agent, and inhibits Wnt/β-catenin pathway.
-
Wnt/β-catenin signaling inhibitor
Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling. -
natural product
L-Quebrachitol is a natural product isolated from many plants, promotes osteoblastogenesis by uppregulation of BMP-2, runt-related transcription factor-2 (Runx2), MAPK (ERK, JNK, p38α), and Wnt/β-catenin signaling pathway. -
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). -
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 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. -
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. -
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. -
Wnt/β-catenin Activator
Astragaloside I is a Wnt/β-catenin activator known for its osteogenic properties. It promotes osteoblast differentiation by enhancing the Wnt/β-catenin signaling pathway. This compound is valuable for research focused on bone development, regeneration, and related signaling mechanisms in various biological systems. -
Wnt/β-catenin Inhibitor
KWZY-11 is a potent Wnt/β-catenin inhibitor that effectively modulates the associated signaling pathway. This compound demonstrates strong biological activity by inducing DNA damage and promoting apoptosis specifically in MDA-MB-231 breast cancer cells. Its dual inhibition of PARP and CDK6 enhances its potential applications in cancer research, particularly for therapeutic strategies targeting tumor cell proliferation. -
β-catenin Inhibitor
β-catenin-IN-9 is a potent inhibitor of β-catenin, a key regulator in various signaling pathways. It has been shown to induce apoptosis and cell cycle arrest, while effectively inhibiting migration, invasion, and epithelial-mesenchymal transition (EMT) in colorectal cancer cells. Additionally, β-catenin-IN-9 suppresses the transcription of β-catenin and vimentin, leading to significant reductions in β-catenin protein levels. This reagent is valuable for research focused on colorectal cancer and related signaling pathways. -
β-catenin Inhibitor
Zolucatetide is a potent inhibitor of β-catenin, demonstrating an IC50 of less than 50 nM. It disrupts the interaction between β-catenin and the T-cell factor (TCF) transcription factor, leading to inhibited cell proliferation and induced cell cycle arrest in sensitive cell lines. In preclinical studies, Zolucatetide exhibits notable anti-tumor efficacy in xenograft models of colon cancer, specifically in COLO320DM cells with APC and TP53 mutations. This compound is valuable for research focused on colon cancer and related pathways. -
β catenin/BCL9 PPI Inhibitor
ZW4864 is a selective inhibitor of the β-catenin/B-Cell lymphoma 9 (BCL9) protein-protein interaction. It demonstrates potent inhibition with a Ki value of 0.76 μM and an IC50 of 0.87 μM. This compound is valuable for research applications targeting the Wnt signaling pathway in cancer biology, particularly in studies related to tumor progression and development. -
β-catenin Inhibitor
NRX-252262 is a potent β-catenin inhibitor that enhances the interaction between β-catenin and its E3 ligase, SCFβ-TrCP, facilitating the degradation of mutant β-catenin. With an EC50 of 3.8 nM, it serves as a valuable tool for studying the Wnt signaling pathway and its implications in various cancers and developmental processes. This compound is useful in research applications focused on β-catenin dysregulation and therapeutic strategies targeting Wnt-mediated pathways. -
β-Catenin Inhibitor
β-Catenin-IN-2 is a potent inhibitor of β-catenin, a key regulator in the Wnt signaling pathway. This compound demonstrates significant biological activity in various cancer models, particularly in the study of colorectal cancer. Research applications include investigating the role of β-catenin in tumorigenesis and exploring potential therapeutic interventions targeting this pathway. -
β-catenin Inhibitor
β-catenin-IN-3 is a selective inhibitor of β-catenin, targeting a cryptic allosteric modulation site with a binding affinity of K D 54.96 nM. This compound effectively reduces the viability of β-catenin-driven cancer cells by promoting degradation of β-catenin through the proteasome pathway. β-catenin-IN-3 is valuable for research applications focused on cancer biology and therapeutic strategies targeting aberrant Wnt signaling. -
β-catenin:β-TrCP Interaction Enhancer
NRX-252114 is a potent enhancer of the β-catenin:β-TrCP interaction, facilitating the binding of phosphorylated β-catenin peptides to the E3 ubiquitin ligase SCFβ-TrCP. With an EC50 of 6.5 nM and a Kd of 0.4 nM, this compound significantly boosts the degradation of mutant β-catenin. NRX-252114 is useful in research applications focused on the Wnt signaling pathway and its implications in cancer biology and developmental processes. -
β-catenin:β-TrCP Interaction Enhancer
NRX-103094 is an enhancer of the β-catenin:β-TrCP interaction, specifically targeting the binding of phospho-Ser33/Ser37 β-catenin to its E3 ligase, SCFβ-TrCP. With an EC50 of 62 nM and a Kd of 0.6 nM, NRX-103094 facilitates this critical protein-protein interaction, making it a valuable tool for research into Wnt signaling pathways and related cellular processes. Its ability to modulate β-catenin stability can aid investigations into various aspects of cellular biology, including cancer research and developmental biology. -
Wnt/β-catenin Signaling Activator
Wnt/β-catenin agonist 2 is a potent activator of the Wnt/β-catenin signaling pathway. This compound effectively stimulates Wnt signaling, making it a valuable tool for investigating the molecular mechanisms underlying diseases associated with aberrant signal transduction. Researchers can utilize this reagent in studies focused on developmental biology, cancer research, and regenerative medicine, where modulation of the Wnt pathway plays a critical role. -
Wnt/β-catenin inhibitor
2,5-Dimethylcelecoxib is a selective Wnt/β-catenin pathway inhibitor that shows promising anticancer activity without inhibiting COX-2. It effectively suppresses cancer cell proliferation by targeting the core elements of this signaling pathway. Additionally, 2,5-Dimethylcelecoxib inhibits T-cell factor-dependent transcriptional activity and downregulates the expression of key Wnt/β-catenin target genes, including cyclin D1 and survivin, making it a valuable tool for cancer research.

