| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| 1g | |||
| Other Sizes |
| Targets |
WIC1 targets the Wnt/β-catenin signaling pathway. It functions as an inhibitor of glycogen synthase kinase 3β (GSK3β), a critical component in the Wnt signaling cascade. By inhibiting GSK3β, WIC1 prevents the phosphorylation and degradation of β-catenin, a key mediator in this signaling pathway. The compound inhibits the phosphorylation of β-catenin Y489 and Tp63 expression.
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| ln Vitro |
In BEAS2B cells, WICl (10 nM, 100 nM, 10 μM, and 100 μM) decreases TFC/LEF luciferase reporter gene activity [1]. WICl (1μM) considerably lessens ABSC edema while WICl (10 nM, 100 nM, 10μM, and 100μM) exhibits modest toxicity [1]. 145 known downstream Wnt signaling target genes, including CCND1, MYC, and CTNNB1, have lower mRNA expression when exposed to WICl[1]. Nuclear localization is decreased by WICl (1μM) [1].
WIC1 is a potent Wnt inhibitor that reduces airway basal stem cell (ABSC) proliferation and induces ciliated epithelial cell differentiation in a model of squamous lung cancer. It inhibits the phosphorylation of β-catenin Y489 and Tp63 expression. The compound demonstrates significant anti-cancer activity by disrupting Wnt-mediated transcriptional activation. WIC1 promotes airway basal stem cell homeostasis. |
| ln Vivo |
In vivo activity of WIC1 has not been extensively reported in the available literature. The compound is used in cancer research and has demonstrated significant anti-cancer activity in preclinical models. Further in vivo studies would be required to evaluate its pharmacokinetics, efficacy, and therapeutic potential in animal models of cancer and other Wnt-driven diseases.
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| Enzyme Assay |
Wnt/β-catenin signaling inhibition is measured using luciferase reporter assays in Wnt-responsive cell lines. Cells stably expressing a Wnt-responsive luciferase reporter are treated with WIC1 at varying concentrations. Luciferase activity is measured, and IC50 values are calculated from dose-response curves. GSK3β activity is assessed using kinase assays, and β-catenin levels are measured by Western blot.
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| Cell Assay |
Cellular activity of WIC1 is evaluated in cancer cell lines and airway basal stem cells. Cells are treated with escalating concentrations of WIC1 for 48-72 hours. Cell viability is measured using CellTiter-Glo or MTT assays. Wnt signaling inhibition is confirmed by measuring β-catenin levels and expression of Wnt target genes by Western blot or qRT-PCR. ABSC proliferation and differentiation are assessed in models of squamous lung cancer.
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| Animal Protocol |
In vivo efficacy of WIC1 would typically be evaluated in xenograft mouse models of Wnt-driven cancers. Tumor-bearing mice would be administered WIC1 orally or intraperitoneally at various doses. Tumor volume would be measured bi-weekly, and tumor growth inhibition calculated. Pharmacodynamic endpoints would include assessment of Wnt signaling inhibition in tumor tissues by immunohistochemistry or Western blot. Such studies have not been extensively reported.
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| ADME/Pharmacokinetics |
WIC1 has a molecular formula of C22H23N3O3 and a molecular weight of 377.44. It is soluble in DMSO (1 mg/mL with ultrasonic and warming). The compound is stored as powder at -20°C for up to 3 years. Its chemical name is N-(4-(4-ethylpiperazin-1-yl)phenyl)-2-oxo-2H-chromene-3-carboxamide. The compound has physicochemical properties suitable for research applications.
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| Toxicity/Toxicokinetics |
Toxicological data for WIC1 are limited to research applications. The compound is for research use only and not intended for therapeutic use. As a Wnt inhibitor, toxicity would be evaluated in the context of the specific cell lines or animal models being studied. Comprehensive toxicology profiling would be required for clinical development.
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| References | |
| Additional Infomation |
WIC1 is a potent Wnt inhibitor that can be used for cancer research. It targets the Wnt/β-catenin signaling pathway by inhibiting GSK3β, preventing β-catenin phosphorylation and degradation. The compound reduces airway basal stem cell proliferation and induces ciliated epithelial cell differentiation. WIC1 demonstrates significant anti-cancer activity by disrupting Wnt-mediated transcriptional activation. It is a valuable tool for studying Wnt signaling in cancer and stem cell biology.
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| Exact Mass |
377.17
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| Elemental Analysis |
C, 70.01; H, 6.14; N, 11.13; O, 12.72
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| CAS # |
943083-58-7
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| Related CAS # |
943083-58-7;
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| Appearance |
Yellow to orange solid powder
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| InChi Key |
YQXKWSNLAVFZJL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H23N3O3/c1-2-24-11-13-25(14-12-24)18-9-7-17(8-10-18)23-21(26)19-15-16-5-3-4-6-20(16)28-22(19)27/h3-10,15H,2,11-14H2,1H3,(H,23,26)
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| Chemical Name |
N-(4-(4-Ethylpiperazin-1-yl)phenyl)-2-oxo-2H-chromene-3-carboxamide
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| Synonyms |
WIC1; WIC-1; WIC 1
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~1.67 mg/mL (~4.42 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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