Wnt

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  1. 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.
  2. PARP inhibitor

    XAV 939 is a TNKS inhibitor (IC50 values are 0.011 and 0.004 μM for TNKS1 and TNKS2 respectively).
  3. 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) .
  4. 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.
  5. 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.
  6. 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.

  7. 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.
  8. 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.
  9. 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.
  10. Wnt/β-catenin signaling inhibitor

    CWP232228, a highly potent selective Wnt/β-catenin signaling inhibitor, antagonizes binding of β-catenin to T-cell factor (TCF) in the nucleus.
  11. TNIK inhibitor

    NCB-0846 is an orally available TNIK inhibitor with an IC50 of 21?nM.
  12. Wnt/β-catenin inhibitor

    PNU-74654 is an inhibitor of Wnt/β-catenin pathway with an IC50 of 129.8 μM in NCI-H295 cell.
  13. 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.
  14. Prodigiosin (Prodigiosine) HCl is a potent proapoptotic agent, and inhibits Wnt/β-catenin pathway.
  15. 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.
  16. ERbeta agonist

    Prinaberel(ERB-041) is a potent and selective ERbeta agonist; being >200-fold selective for ERbeta.
  17. 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.
  18. 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.
  19. 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.
  20. 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.
  21. 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.
  22. 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.
  23. 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.
  24. 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).
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. Wnt inhibitor

    IWP-2 is an inactivator of Porcn function and inhibitor of Wnt production, and blocks beta-catenin accumulation. Wnt/b-catenin ('canonical') pathway maintains transcriptional programs that enable stem cells to remain multipotent.
  33. 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).
  34. Prodigiosin (Prodigiosine) is a secondary metabolite of Symbiotic bacteria, with anti-fungal and anti-cancer activity.
  35. PORCN inhibitor

    IWP-L6 is a potent inhibitor of Porcupine (Porcn), a membrane-bound O-acyltransferase (MBOAT) (EC50 = 0.5 nM).
  36. Wnt inhibitor

    Pyrvinium pamoate is an FDA-approved antihelmintic drug that inhibits WNT pathway signaling.
  37. Potent porcupine inhibitor

    Porcn-IN-1 is potent porcupine inhibitor with an IC50 of 0.5??0.2 nM.
  38. Wnt/β-catenin activator

    HLY78 is an activator of the Wnt/β-catenin signaling pathway, which targets the DIX domain of Axin and potentiates the Axin-LRP6 association to promote Wnt signaling transduction.
  39. Heparan sulfate, a complex and linear polysaccharide, exists as part of glycoproteins named heparan sulfate proteoglycans, which are expressed abundantly on the cell surface and in the extracellular matrix.
  40. Wnt/beta-catenin modulator

    KY1220 is a compound that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway; with an IC50 of 2.1 μM in HEK293 reporter cells.
  41. EMT inhibitor-1 is an inhibitor of of Hippo, TGF-β, and Wnt signaling pathways with antitumor activities.
  42. Wnt/β-catenin agonist

    Wnt/β-catenin agonist 1 is a Wnt/β-catenin signalling pathway agonist, with an EC50 of 0.27 μM.
  43. 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.
  44. Wnt inhibitor

    Adavivint (SM04690; Lorecivivint) is a potent and selective inhibitor of canonical Wnt signaling, with an EC50 of 19.5 nM via a high-throughput TCF/LEF-reporter assay in SW480 colon cancer cells.
  45. Wnt/β-catenin signaling inhibitor

    DK419 is a potent and orally active Wnt/β-catenin signaling inhibitor, with an IC50 of 0.19 μM. DK419 reduces protein lelvels of Axin2, β-catenin, c-Myc, Cyclin D1 and Survivin and induces production of pAMPK.
  46. Salinomycin is an antibacterial and coccidiostat ionophore therapeutic drug.
  47. 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.
  48. Wnt inhibitor

    CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with IC50 value of 5 nM.
  49. 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.
  50. Wnt/beta-catenin inhibitor

    KYA1797K is a highly potent and selective Wnt/beta-catenin inhibitor with IC50 of 0.75 μM (TOPflash assay).

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