Conditionnement : 10mg
Synonyms: IWR-1-endo, endo-IWR 1
| Description | IWR-1 (IWR-1-endo) is a tankyrase inhibitor that targets the Wnt/β-catenin pathway, with an IC50 of 180 nM. IWR-1 contributes to the activation of TCF/LEF and the expression of downstream targets of the Wnt/β-catenin pathway. IWR-1 promotes β-catenin phosphorylation by enhancing the stability of the Axin-mediated disassembly complex. IWR-1 can be used in research on diseases such as cancer and psoriasis. |
| Targets & IC50 | HT29 cells:24.4 μM, SW48 cells:2.5 μM (EC50), SW48 cells:0.25 μM, Wnt:0.2 μM (EC50), HEK293T cells:26 nM |
| In vitro | Methods: Human colorectal cancer cell lines HCT116 and HT29 were treated with IWR-1 at concentrations of 5, 10, 20, and 50 μM for 24 and 48 hours. Cell proliferation was assessed using the MTT/CCK-8 assay. Results: IWR-1 exhibited concentration- and time-dependent inhibition of cell proliferation. [1] |
| In vivo | Methods: Psoriasiform skin inflammation was induced in Balb/c mice by applying imiquimod cream to the dorsal skin daily for 5 consecutive days. On days 1, 3, and 5, mice received subcutaneous injections of IWR-1 (10 mg/kg) or IL-36γ (2 μg/mouse). After the fifth day of treatment, mice were euthanized, and dorsal skin tissue was harvested for subsequent analysis. Results: IL-36γ treatment significantly exacerbated IMQ-induced PASI scores, while IWR-1 treatment significantly suppressed IL-36γ-induced increases in PASI scores. [2] |
| Synonyms | IWR-1-endo, endo-IWR 1 |
| Molecular Weight | 409.44 |
| Formula | C25H19N3O3 |
| Cas No. | 1127442-82-3 |
| Smiles | O=C(Nc1cccc2cccnc12)c1ccc(cc1)N1C(=O)C2C3CC(C=C3)C2C1=O |
| Relative Density. | 1.425 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 85.8 mg/mL (209.55 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4.1 mg/mL (10.01 mM), Suspension. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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