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IWP-2

Cat. No. M2237
IWP-2 Structure
Synonym:

Inhibitor of Wnt Production-2

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 45  USD45 In stock
10mg USD 70  USD70 In stock
50mg USD 250  USD250 In stock
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Quality Control
Biological Activity

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.

Product Citations
Customer Product Validations & Biological Datas
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
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
Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 466.6
Formula C22H18N4O2S3
CAS Number 686770-61-6
Purity >98%
Solubility DMSO 2 mg/mL
DMF 8 mg/mL
Storage at -20°C
References

[1] Balbina Garcia-Reyes, et al. J Med Chem. Discovery of Inhibitor of Wnt Production 2 (IWP-2) and Related Compounds As Selective ATP-Competitive Inhibitors of Casein Kinase 1 (CK1) δ/ε

[2] George Maiti, et al. Proc Natl Acad Sci U S A. The Wingless homolog Wnt5a stimulates phagocytosis but not bacterial killing

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Keywords: IWP-2, Inhibitor of Wnt Production-2 supplier, Wnt/beta-catenin, inhibitors

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