IWP-4
Based on 2 publication(s) in Google Scholar
IWP-4 is a Wnt inhibitor with an IC50 of 25 nM. IWP-4 specifically inhibits casein kinase 1δ/ε (CK1δ/ε), with an IC50 of 1.06 μM against wild-type CK1δ, 1.02 μM against the CK1δ kinase domain, and 7.07 μM against CK1ε; it shows enhanced inhibitory activity against the M82F CK1δ mutant (IC50 = 0.14 μM). IWP-4 is applicable to research related to cancer, Alzheimer's disease (AD), and heart failure.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.81%
- No. CAS: 686772-17-8
- Fòrmula: C23H20N4O3S3
- Peso molecular:496.62
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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iCRT3Wnt/β-Catenin Inhibitor
Publications Citing Use of MedChemExpress (MCE) IWP-4
More
Customer Validation & Images
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RT-PCR
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WB
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Cell Imaging/Staining
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Cell Proliferation/Viability Assay
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IF
Actividad biológica
Descripciòn
IC50 & Target
IC50: 25 nM (Wnt)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CAPAN-1 | EC50 |
0.23 μM
Compound: IWP-4
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Antiproliferative activity against human Capan1 cells after 48 hrs by MTT assay
Antiproliferative activity against human Capan1 cells after 48 hrs by MTT assay
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[PMID: 29630366] |
| HEK293 | EC50 |
0.28 μM
Compound: IWP-4
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Antiproliferative activity against human HEK293 cells after 48 hrs by MTT assay
Antiproliferative activity against human HEK293 cells after 48 hrs by MTT assay
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[PMID: 29630366] |
| HT-29 | EC50 |
0.34 μM
Compound: IWP-4
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Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay
Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay
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[PMID: 29630366] |
| MIA PaCa-2 | EC50 |
0.23 μM
Compound: IWP-4
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Antiproliferative activity against human MIAPaCa2 cells after 48 hrs by MTT assay
Antiproliferative activity against human MIAPaCa2 cells after 48 hrs by MTT assay
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[PMID: 29630366] |
| PANC-1 | EC50 |
0.23 μM
Compound: IWP-4
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Antiproliferative activity against human PANC1 cells after 48 hrs by MTT assay
Antiproliferative activity against human PANC1 cells after 48 hrs by MTT assay
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[PMID: 29630366] |
| SW-620 | EC50 |
0.23 μM
Compound: IWP-4
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Antiproliferative activity against human SW620 cells after 48 hrs by MTT assay
Antiproliferative activity against human SW620 cells after 48 hrs by MTT assay
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[PMID: 29630366] |
In Vitro
IWP-4 (48 h) inhibits the proliferation of all tested cancer cell lines, with submicromolar EC50 values ranging from 0.23 μM to 0.93 μM[1].
IWP-4 (1 μM; 24 h) antagonizes the protective effect of Ginkgolide B (HY-N0784) on primary rat cortical astrocytes against glutamate-induced injury by reversing Ginkgolide B-mediated regulation of apoptosis-related genes and proteins, as well as glutamate transporter genes and proteins[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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No. CAS 686772-17-8
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Appearance Solid
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Peso molecular 496.62
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Fòrmula C23H20N4O3S3
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Color White to light yellow
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SMILES
O=C(NC1=NC2=CC=C(C)C=C2S1)CSC3=NC(CCS4)=C4C(N3C5=CC=CC=C5OC)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Chin Med
Astragalus membranaceus (Huangqi) and Rhizoma curcumae (Ezhu) decoction suppresses colorectal cancer via downregulation of Wnt5/β-Catenin signal. [Abstract]2022 Jan 6;17(1):11. PMID: 34991661
IWP-4 purchased from MedChemExpress. Usage Cited in: Chin Med. 2022 Jan 6;17(1):11. [Abstract]
IWP-4 (24 h) significantly reduced the mRNA levels of Wnt 5, β-Catenin, ARF6, and N-Cadherin, compared with the AR-CS alone group in SW620 cells.
IWP-4 purchased from MedChemExpress. Usage Cited in: Chin Med. 2022 Jan 6;17(1):11. [Abstract]
IWP-4 (24 h) significantly reduced theprotein levels of Wnt 5, β-Catenin, ARF6, and N-Cadherin, compared with the AR-CS alone group in SW620 cells.
IWP-4 purchased from MedChemExpress. Usage Cited in: Chin Med. 2022 Jan 6;17(1):11. [Abstract]
IWP-4 (24 h) enhanced the inhibitory effect of AR-CS on the migration of SW620 cells.
IWP-4 purchased from MedChemExpress. Usage Cited in: Chin Med. 2022 Jan 6;17(1):11. [Abstract]
IWP-4 (24 h) enhanced the inhibitory effect of AR-CS on the proliferation of SW620 cells.
IWP-4 purchased from MedChemExpress. Usage Cited in: Chin Med. 2022 Jan 6;17(1):11. [Abstract]
IWP-4 (24 h) increased the fluorescence intensity of β-Catenin in SW620 cells.
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Biol Pharm Bull
5-Demethylnobiletin Ameliorates Isoproterenol-Induced Cardiac Fibrosis and Apoptosis by Repressing the Sirt1/FOXO3a/NF-κB and Wnt/β-Catenin Pathways. [Abstract]2024;47(10):1774-1785. PMID: 39477471
Solvente y solubilidad
In Vitro:
DMSO : 1.72 mg/mL (3.46 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocolo
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Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. García-Reyes B, et al. Discovery of Inhibitor of Wnt Production 2 (IWP-2) and Related Compounds As Selective ATP-Competitive Inhibitors of Casein Kinase 1 (CK1) δ/ε. J Med Chem. 2018;61(9):4087-4102. [Content Brief]
[2]. Wang J, et al. A RNA-seq approach for exploring the protective effect of ginkgolide B on glutamate-induced astrocytes injury. J Ethnopharmacol. 2021;270:113807. [Content Brief]
[3]. Hudson J, et al. Primitive cardiac cells from human embryonic stem cells. Stem Cells Dev. 2012 Jun 10;21(9):1513-23. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0136 mL | 10.0681 mL | 20.1361 mL | 50.3403 mL |
IWP-4 Related Classifications
HY-12879 Related Classifications
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