IWP-3
Based on 1 Customer Validation
IWP-3 is a Wnt production inhibitor with an IC50 of 40 nM. IWP-3 also acts as a CK1δ inhibitor, with an IC50 of 1.89 μM against rat full-length CK1δ. IWP-3 inhibits the function of Porcupine (Porcn), thereby blocking the palmitoylation of Wnt proteins, suppressing the canonical Wnt signaling pathway, reducing the proliferative capacity of cancer cells, promoting the differentiation of mesoderm into cardiomyocytes and increasing cardiomyocyte yield. IWP-3 reduces embryonic cell division, alters the cell movement along the anterior-posterior axis of embryos, and causes embryonic shortening. IWP-3 can be used in studies related to cancers such as pancreatic cancer.
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- Pureza: 98.10%
- No. CAS: 687561-60-0
- Fòrmula: C22H17FN4O2S3
- Peso molecular:484.59
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Actividad biológica
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CK1δ 1.89 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CAPAN-1 | EC50 |
>10 μM
Compound: IWP-3
|
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 |
3.5 μM
Compound: IWP-3
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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
|
[PMID: 29630366] |
| HEK-293T | IC50 |
538 nM
Compound: 3, IWP-3
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Inhibition of beta-casein-dependent canonical Wnt3 pathway in human HEK293T cells by luciferase reporter gene assay
Inhibition of beta-casein-dependent canonical Wnt3 pathway in human HEK293T cells by luciferase reporter gene assay
|
[PMID: 22191557] |
| HT-29 | EC50 |
>10 μM
Compound: IWP-3
|
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
|
[PMID: 29630366] |
| MIA PaCa-2 | EC50 |
5.34 μM
Compound: IWP-3
|
Antiproliferative activity against human MIAPaCa2 cells after 48 hrs by MTT assay
Antiproliferative activity against human MIAPaCa2 cells after 48 hrs by MTT assay
|
[PMID: 29630366] |
| PANC-1 | EC50 |
4.87 μM
Compound: IWP-3
|
Antiproliferative activity against human PANC1 cells after 48 hrs by MTT assay
Antiproliferative activity against human PANC1 cells after 48 hrs by MTT assay
|
[PMID: 29630366] |
| SW-620 | EC50 |
8.62 μM
Compound: IWP-3
|
Antiproliferative activity against human SW620 cells after 48 hrs by MTT assay
Antiproliferative activity against human SW620 cells after 48 hrs by MTT assay
|
[PMID: 29630366] |
IWP-3 potently induces cardiogenesis in day 4 mesodermal cells derived from human embryonic stem cells, with an EC50 of 1214 nM. It drives mesodermal progenitor cells to form cardiomyocytes without expanding other mesodermal lineages[1].
IWP-3 (10 μM) does not inhibit the kinase activity of bovine GST-CK1α, exerts moderate inhibitory effects on the kinase activities of human GST-CK1γ3 and human CK1ε, and significantly inhibits the purified kinase activities of rat GST-CK1δ and rat CK1δKD[2].
IWP-3 inhibits purified rat CK1δKD, GST-wtCK1δ and GST-M82FCK1δ with IC50 values of 0.55 μM, 1.89 μM and 0.15 μM, respectively[2].
IWP-3 (0.313 μM-10 μM; 48 h) inhibits the proliferation of MiaPaCa2, Panc-1, Panc-89, HEK293 and SW620 cancer cell lines, with EC50 values ranging from 3.50 μM to 8.62 μM; in contrast, it exerts no inhibitory effect on the proliferation of A818-6, HT29 and Capan1 cells even at concentrations as high as 10 μM[2].
IWP-3 (0.45-45 µM; 1-4 h) causes significant shortening of germband length at 2 h and 3 h of incubation and a significant reduction in cell proliferation at 2 h of incubation when applied to dissected Tribolium castaneum EFA-nGFP transgenic embryos[3].
IWP-3 (45 µM; 2 h) significantly reduces total cell displacement and net cell movement across all germband regions, and decreases the proportion of cells moving along the anterior-posterior axis during 2-hour live-cell imaging when treated on dissected Tribolium castaneum EFA-nGFP transgenic embryos[3].
IWP-3 is a Wnt production inhibitor with an IC50 of 40 nM; it blocks palmitoylation of Wnt protein by inhibiting Porcn[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 687561-60-0
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Appearance Solid
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Peso molecular 484.59
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Fòrmula C22H17FN4O2S3
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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=C(F)C=C5)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 16.67 mg/mL (34.40 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (276 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]. Willems E, et al. Small-molecule inhibitors of the Wnt pathway potently promote cardiomyocytes from human embryonic stem cell-derived mesoderm. Circulation research. 2011 Aug 05;109(4):360-4. [Content Brief]
[2]. 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. Journal of medicinal chemistry. 2018 May 10;61(9):4087-4102. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0636 mL | 10.3180 mL | 20.6360 mL | 51.5900 mL |
| 5 mM | 0.4127 mL | 2.0636 mL | 4.1272 mL | 10.3180 mL | |
| 10 mM | 0.2064 mL | 1.0318 mL | 2.0636 mL | 5.1590 mL | |
| 15 mM | 0.1376 mL | 0.6879 mL | 1.3757 mL | 3.4393 mL | |
| 20 mM | 0.1032 mL | 0.5159 mL | 1.0318 mL | 2.5795 mL | |
| 25 mM | 0.0825 mL | 0.4127 mL | 0.8254 mL | 2.0636 mL | |
| 30 mM | 0.0688 mL | 0.3439 mL | 0.6879 mL | 1.7197 mL |