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.
Cell Experiment | |
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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 | |
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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 |
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
Molecular Weight | 466.6 |
Formula | C22H18N4O2S3 |
CAS Number | 686770-61-6 |
Purity | >99% |
Solubility | DMSO |
Storage | at -20°C |
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