IWP-2 is an inhibitor of Wnt production. IWP-2 inactivates Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion. IWP-2 selectively inhibits palmitoylation of Wnt, and blocks Wnt-dependent phosphorylation of Lrp6 receptor and Dvl2, and β-catenin accumulation. IWP-2 is useful in both suppressing embryonic stem cell self-renewal and decreasing cancer cell proliferation, migration and invasion.
Chem Biol Interact. 2023 Dec 1;386:110777.
Assessment of doxorubicin toxicity using human cardiac organoids: A novel model for evaluating drug cardiotoxicity
IWP-2 purchased from AbMole
Stem Cell Reports. 2021 Jun 8;16(6):1568-1583.
Photobiomodulation therapy for hair regeneration: A synergetic activation of β-CATENIN in hair follicle stem cells by ROS and paracrine WNTs
IWP-2 purchased from AbMole
Oncol Rep. 2020 Aug;44(2):577-588.
TNF‑α promotes the malignant transformation of intestinal stem cells through the NF‑κB and Wnt/β‑catenin signaling pathways
IWP-2 purchased from AbMole
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Source | ONCOLOGY REPORTS (2020 Aug). Figure 6. IWP-2 (Abmole Bioscience, US) |
| Method | western blot | |
| Cell Lines | NCM460s cells | |
| Concentrations | 1, 10, 100 µM | |
| Incubation Time | 3 h | |
| Results | Notably, IWP-2 also counteracted TNF-α-induced activation of the NF-κB pathway in NCM460s cells, including increased phosphorylation of IKKα/β and IκBα, decreased protein levels of IκBα and nuclear translocation of p65 |
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Source | Front Immunol (2018). Figure 6. IWP-2 |
| Method | injected intravenously | |
| Cell Lines | C57BL/6 mice | |
| Concentrations | 20 mg/kg | |
| Incubation Time | 4.5 h | |
| Results | This view is supported by reduced percentages of IFN-γ+ liver CD3+NK1.1+ cells in mice treated with IWP-2, a small molecule inhibitor of the acyltransferase Porcupine, which plays a central role in Wnt secretion |
| Cell Experiment | |
|---|---|
| Cell lines | MKN28 cell line |
| Preparation method | Cell proliferation assay CellTiter 96 Aqueous Non-Radioactive Cell Proliferation Assay kit (Promega Corporation, Madison, WI, USA) was used. Transwell migration and invasion assay Haptotaxis chambers (8-μm pore size, Corning Costar, Cambridge, MA, USA) without or with 5 mg/ml matrigel (Sigma Aldrich) were used for migration and invasion assays, respectively. The experiments were repeated three times independently. |
| Concentrations | 0,5,10,20,50µM |
| Incubation time | 5 days |
| Animal Experiment | |
|---|---|
| Animal models | six month-old zebrafish model |
| Formulation | 0.1% DMSO |
| Dosages | 10 μM |
| Administration | in aquarium water supplemented with 10 μM IWR-1 or in 0.1% DMSO as a control |
| Molecular Weight | 466.6 |
| Formula | C22H18N4O2S3 |
| CAS Number | 686770-61-6 |
| Solubility (25°C) | DMSO 2 mg/mL DMF 8 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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| FZD7 antagonist 1
FZD7 antagonist 1 (peptide 34) is a dFz7-21 analogue. |
| NLS-StAx-h
NLS-StAx-h is a selective, cell permeable, stapled peptide Wnt signaling inhibitor with an IC50 of 1.4 μM. |
| Zamaporvint
Zamaporvint is an orally active, selective Wnt inhibitor that targets the membrane-bound o-acyltransferase porcupine and inhibits Wnt ligand palmitoylation, secretion and pathway activation. In addition, Zamaporvint displays potent antiproliferative effects in Wnt ligand-dependent colorectal and pancreatic cell lines. It can be used in cancer-related studies. |
| Foxy-5
Foxy-5, a WNT5A agonist and a mimetic peptide of WNT5A, triggers cytoplasmic free calcium signaling without affecting β-catenin activation and inhibits migration and invasion of epithelial cancer cells.Foxy-5 effectively reduces metastatic spread of prostate cancer cells with low WNT5A expression in an in situ mouse model. |
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