Wnt-C59 (Synonyms: PORCN Inhibitor II) |
| Catalog No.GC13658 |
Wnt-C59 (C59) es un inhibidor oral de puercoespÍn (PORCN) muy potente con una IC50 de 74 pM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1243243-89-1
Sample solution is provided at 25 µL, 10mM.
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Wnt-C59 is a highly potent inhibitor of Porcupine (Porcn), a member of the Mboat (membrane-bound O-acyl deglycosylase) family, with an IC50 value of 74pM, and can inhibit Wnt signaling[1]. The Wnt signaling pathway is a complex network of proteins whose functions are most commonly seen in embryonic development and cancer, but are also involved in normal physiological processes in adult animals[2]. Wnt-C59 has the potential to eradicate cancer stem cells (CSCs) in human tumors[3]. Wnt-C59 can be used to induce human pluripotent stem cells (IPSCs) to differentiate into cortical motor neurons (CMNs) or their progenitors[4].
In vitro, Wnt-C59 (0.01, 1μM) treatment of NIH 3T3 fibroblasts for 48h significantly induced the expression of genes related to hypertrophy (BNP) and fibrosis (COL1 and COL3) in the cells[5]. Wnt-C59 (10μM) treatment of human fetal liver progenitor cells (HFLPC) significantly inhibited cell migration and proliferation induced by Wnt3a and Wnt5a[6].
In vivo, Wnt-C59 (5mg/kg) was orally treated for 4 weeks in cardiac hypertrophy model mice, which significantly improved the cardiac function and survival rate of mice, and attenuated the transverse aortic constriction (TAC)-induced cardiac mass, increase in cardiomyocyte cross-sectional area, cardiac fibrosis, cardiomyocyte apoptosis, and expression of hypertrophic biomarkers β-MHC, ANP, and BNP[7]. Wnt-C59 (40, 60mg/kg) was intraperitoneally treated in mice with endotoxin-induced sepsis, which significantly improved the survival rate of mice and reduced the lethality and plasma levels of proinflammatory cytokines and organ damage biomarkers[8].
References:
[1] Shah K, Panchal S, Patel B. Porcupine inhibitors: Novel and emerging anti-cancer therapeutics targeting the Wnt signaling pathway[J]. Pharmacological research, 2021, 167: 105532.
[2] Anastas J N, Moon R T. WNT signalling pathways as therapeutic targets in cancer[J]. Nature Reviews Cancer, 2013, 13(1): 11-26.
[3] Cheng Y, Phoon Y P, Jin X, et al. Wnt-C59 arrests stemness and suppresses growth of nasopharyngeal carcinoma in mice by inhibiting the Wnt pathway in the tumor microenvironment[J]. Oncotarget, 2015, 6(16): 14428.
[4] Motono M, Ioroi Y, Ogura T, et al. WNT-C59, a small-molecule WNT inhibitor, efficiently induces anterior cortex that includes cortical motor neurons from human pluripotent stem cells[J]. Stem cells translational medicine, 2016, 5(4): 552-560.
[5] Paul M A, Wainwright C L, Hector E E, et al. Short‐Term Oral Administration of the Porcupine Inhibitor, Wnt‐c59, Improves the Structural and Functional Features of Experimental HFpEF[J]. Pharmacology Research & Perspectives, 2025, 13(1): e70054.
[6] Liu Z, Kuna V K, Xu B, et al. Wnt ligands 3a and 5a regulate proliferation and migration in human fetal liver progenitor cells[J]. Translational Gastroenterology and Hepatology, 2021, 6.
[7] Zhao Z, Liu H, Li Y, et al. Wnt-C59 attenuates pressure overload-induced cardiac hypertrophy via interruption of wnt pathway[J]. Medical Science Monitor: International Medical Journal of Experimental and Clinical Research, 2020, 26: e923025-1.
[8] Jang J, Song J, Sim I, et al. Wnt-Signaling Inhibitor Wnt-C59 suppresses the cytokine upregulation in multiple organs of lipopolysaccharide-induced endotoxemic mice via reducing the interaction between β-Catenin and NF-κB[J]. International Journal of Molecular Sciences, 2021, 22(12): 6249.
| Cell experiment [1]: | |
Cell lines | NIH 3T3 fibroblasts |
Preparation Method | NIH 3T3 fibroblasts were seeded in 6 well plates (50000 cells per well) and treated with Wnt-C59 (0.01μM and 1μM) for 48h and the expression of genes related to hypertrophy (BNP) and fibrosis (Col1 and Col3) measured in cell lysates. |
Reaction Conditions | 0.01, 1μM; 48h |
Applications | Wnt-C59 induced the expression of BNP and both Col1 and Col3 in Fibroblasts. |
| Animal experiment [2]: | |
Animal models | C57BL/6J mice |
Preparation Method | Mice were divided into 4 groups: sham, sham+Wnt-C59, transverse aortic constriction (TAC), and TAC+Wnt-C59. Briefly, mice were anesthetized with isoflurane (2%) and a sternotomy was performed to visualize the aortic arch. Then, 7-0 polypropylene suture was used to ligate the aortic arch with a 27G needle as a space holder, which was subsequently removed. The same surgical procedures except for the ligation of the aorta were performed to animals in the sham group. Wnt-C59 was dissolved in saline and administered daily by oral gavage (5mg/kg/day) for experimental groups for 4 weeks. Cardiac function was measured by transthoracic echocardiography using GE vivid 8-dimension ultrasound 4 weeks after TAC surgery. Then mice were anesthetized by isoflurane overdose and hearts were harvested. |
Dosage form | 5mg/kg; for 4 weeks; p.o. |
Applications | Wnt-C59 significantly improved cardiac function and enhanced survival of mice subjected to TAC surgery. Histologically, Wnt-C59 attenuated TAC-induced increase in heart mass, cross-section area of cardiomyocyte, cardiac fibrosis, cardiomyocyte apoptosis, and expression of the hypertrophic biomarkers β-MHC, ANP, and BNP. |
References: | |
| Cas No. | 1243243-89-1 | SDF | |
| Sinónimos | PORCN Inhibitor II | ||
| Chemical Name | 2-[4-(2-methylpyridin-4-yl)phenyl]-N-(4-pyridin-3-ylphenyl)acetamide | ||
| Canonical SMILES | CC1=NC=CC(=C1)C2=CC=C(C=C2)CC(=O)NC3=CC=C(C=C3)C4=CN=CC=C4 | ||
| Formula | C25H21N3O | M.Wt | 379.45 |
| Solubility | ≥ 18.95mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6354 mL | 13.177 mL | 26.3539 mL |
| 5 mM | 0.5271 mL | 2.6354 mL | 5.2708 mL |
| 10 mM | 0.2635 mL | 1.3177 mL | 2.6354 mL |
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- Purity: >99.50%
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Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)
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