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Catalog No.
Product Name
Application
Product Information
Citations
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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).- 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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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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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
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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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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 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). -
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. -
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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Potent porcupine inhibitor
Porcn-IN-1 is potent porcupine inhibitor with an IC50 of 0.5??0.2 nM. -
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. -
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. -
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. -
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. -
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. -
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/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 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. -
WNT Inhibitor
WNTinib is a selective WNT signaling inhibitor targeting mutated β-catenin (CTNNB1) in hepatocellular carcinoma (HCC). By effectively disrupting the oncogenic Wnt pathway, WNTinib inhibits key kinases such as KIT and MAPK, leading to the reduction of EZH2 activation. This compound is suitable for research applications focused on cancer biology and the mechanisms of liver tumorigenesis. -
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. -
wnt/β-catenin Inhibitor
Teplinovivint is a selective inhibitor of the Wnt/β-catenin signaling pathway. It exhibits significant anti-inflammatory properties and is valuable for research related to tendinopathy and related musculoskeletal disorders. This compound serves as a critical tool for investigating the roles of Wnt signaling in various biological processes and diseases. -
Wnt/β-Catenin Inhibitor
YW1128 is a potent Wnt/β-Catenin inhibitor that induces the proteasomal degradation of β-catenin, leading to the inhibition of Wnt/β-Catenin signaling pathways in cells. This compound significantly reduces hepatic lipid accumulation and enhances glucose tolerance in mice subjected to a high-fat diet, demonstrating an absence of noticeable toxicity. Furthermore, YW1128 downregulates genes associated with glucose and fatty acid anabolism, making it a valuable tool for research into metabolic disorders and Wnt signaling pathway modulation. -
Wnt/β-catenin Signaling Pathway Inhibitor
Wnt/β-catenin-IN-2 is an inhibitor of the Wnt/β-catenin signaling pathway, displaying an IC50 value of 7.1 μM and a KD value of 2.5 μM. This compound is useful in cancer research, enabling the study of Wnt/β-catenin pathway modulation and its implications in tumorigenesis. Its application can enhance understanding of the mechanistic roles of this pathway in various malignancies. -
Wnt Inhibitor
PTK7/β-catenin-IN-2 is a potent inhibitor of the PTK7/β-catenin interaction, effectively disrupting Wnt/β-catenin signaling with an IC50 of 5.6 μM. This inhibition impairs cell growth mediated by the Wnt pathway and demonstrates potential anticancer activity. Additionally, PTK7/β-catenin-IN-2 exhibits inhibitory effects on the p53-MDM2 interaction, with an IC50 of 157.1 μM, making it valuable for research focused on cancer therapies and signaling pathway modulation. -
Wnt/β-catenin Signal Inhibitor
KP-6 is a polypeptide that acts as a Wnt/β-catenin signaling pathway inhibitor. By inhibiting TGF-β, KP-6 disrupts critical fibrotic signaling pathways in vivo, effectively reducing renal tissue damage and fibrotic progression. This compound holds promise for research focused on chronic kidney disease (CKD) and other fibrosis-related disorders, making it a valuable tool for studying disease mechanisms and potential therapeutic interventions. -
Wnt/β-catenin Inhibitor
Wnt/β-catenin-IN-5 is a potent inhibitor of the Wnt/β-catenin signaling pathway. This compound demonstrates significant inhibition of cell proliferation in HCT 116, SW480, and A549 cell lines, with IC50 values of 3.05 μM, 3.27 μM, and 34.91 μM, respectively. It serves as a valuable tool for research focused on cancer biology and the role of Wnt signaling in tumor development and progression. -
Wnt/β-catenin Inhibitor
Wnt/β-catenin-IN-3 is a potent inhibitor of the Wnt/β-catenin signaling pathway, demonstrating low micromolar GI50 values across various cancer cell lines. This compound induces G2/M cell cycle arrest by activating the p53-p21 pathway and promotes apoptotic cell death through both intrinsic and extrinsic mechanisms in colon cancer cells. It serves as a valuable tool for investigating the role of Wnt/β-catenin signaling in cancer biology and therapeutic applications. -
Wnt/β-catenin Inhibitor
Getacatetide is a peptide-based inhibitor of the Wnt/β-catenin signaling pathway. This compound is designed to interfere with the activation of Wnt target genes, making it a valuable tool for investigating the role of Wnt/β-catenin signaling in solid tumors. Getacatetide's ability to disrupt this pathway facilitates research into cancer biology and the development of potential therapeutic strategies. -
Wnt Inhibitor
Halofenate acts as a Wnt inhibitor, impacting the Wnt signaling pathway crucial for cell proliferation and differentiation. It demonstrates significant biological activity by effectively reducing serum triglyceride levels by 50% in hypertriglyceridemic patients and decreasing serum uric acid by 30%, highlighting its potential uricosuric effects. Halofenate additionally increases plasma thyroxine (T4) levels, suggesting implications for thyroid function regulation, supported by in vitro studies showing its ability to displace T4 from thyroid-binding proteins. This compound can be valuable for research into metabolic disorders and thyroid function modulation. -
Wnt Inhibitor
Jatrophone is a diterpenoid that functions as a Wnt inhibitor, exhibiting significant anticancer activity. Isolated from Jatropha isabelli, Jatrophone disrupts the Wnt/β-catenin signaling pathway, leading to a reduction in cell proliferation and inhibition of epithelial-mesenchymal transition (EMT) in triple-negative breast cancer cells. This compound is valuable for research focused on cancer biology and therapeutic strategies targeting Wnt pathway modulation.
