ETC-159
Based on 8 publication(s) in Google Scholar
ETC-159 (ETC-1922159) is a potent, orally available PORCN inhibitor. ETC-159 inhibits β-catenin reporter activity with an IC50 of 2.9 nM.
For research use only. We do not sell to patients.
- Purity: 99.13%
- CAS No.: 1638250-96-0
- Formula: C19H17N7O3
- Molecular Weight:391.38
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) ETC-159
More- Sci Adv. 2020 May 22;6(21):eaaz5913. [Abstract]
- Cell Rep. 2023 May 23;42(6):112546. [Abstract]
- Eur J Pharmacol. 2023 Apr 15:945:175628. [Abstract]
- Sci Rep. 2026 Mar 5. [Abstract]
- Cell Transplant. 2023 Jan-Dec:32:9636897231212746. [Abstract]
- Am J Physiol Endocrinol Metab. 2021 May 1;320(5):E951-E966. [Abstract]
- Npj Viruses. 2024 Feb 21;2(1):6. [Abstract]
- PRACTICAL ONCOLOGY JOURNAL. 2018,32(02):103-106.
Customer Validation & Images
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WB
Biological Activity
IC50: 2.9 nM (β-catenin)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
2.9 nM
Compound: ETC159
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Inhibition of porcupine in human HEK293 cells assessed as reduction in Wnt secretion by measuring suppression of beta-catenin reporter activity after 24 hrs by STF reporter assay
Inhibition of porcupine in human HEK293 cells assessed as reduction in Wnt secretion by measuring suppression of beta-catenin reporter activity after 24 hrs by STF reporter assay
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[PMID: 26522946] |
| HT-1080 | IC50 |
18.1 nM
Compound: ETC159
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Inhibition of mouse porcupine expressed in human HT1080 cells assessed as reduction in beta catenin reporter activity using firefly luciferase substrate STF reporter assay
Inhibition of mouse porcupine expressed in human HT1080 cells assessed as reduction in beta catenin reporter activity using firefly luciferase substrate STF reporter assay
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[PMID: 26522946] |
| HT-1080 | IC50 |
70 nM
Compound: ETC159
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Inhibition of xenopus porcupine expressed in human HT1080 cells assessed as reduction in beta catenin reporter activity using firefly luciferase substrate STF reporter assay
Inhibition of xenopus porcupine expressed in human HT1080 cells assessed as reduction in beta catenin reporter activity using firefly luciferase substrate STF reporter assay
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[PMID: 26522946] |
ETC-159 blocks the secretion and activity of all Wnts. ETC-159 has robust activity in multiple cancer models driven by high Wnt signaling. ETC-159 is highly efficacious in molecularly defined colorectal cancers (CRCs) with R-spondin translocations[1]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1638250-96-0
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Appearance Solid
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Molecular Weight 391.38
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Formula C19H17N7O3
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Color White to off-white
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SMILES
O=C(NC1=CC=C(C2=CC=CC=C2)N=N1)CN3C=NC4=C3C(N(C)C(N4C)=O)=O
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Synonyms
ETC-1922159
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
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Journal Impact Factor
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Most Recent
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Sci Adv
Combinatorial screening of biochemical and physical signals for phenotypic regulation of stem cell-based cartilage tissue engineering. [Abstract]2020 May 22;6(21):eaaz5913. PMID: 32494742 -
Cell Rep
2023 May 23;42(6):112546. PMID: 37224015 -
Eur J Pharmacol
Novel PORCN inhibitor WHN-88 targets Wnt/β-catenin pathway and prevents the growth of Wnt-driven cancers. [Abstract]2023 Apr 15:945:175628. PMID: 36858339 -
Sci Rep
WNT inhibition activates interferon stimulated gene expression by alleviating epigenetic repression of endogenous retroviruses. [Abstract]2026 Mar 5. PMID: 41781472 -
Cell Transplant
Telocyte-Derived Exosomes Provide an Important Source of Wnts That Inhibits Fibrosis and Supports Regeneration and Repair of Endometrium. [Abstract]2023 Jan-Dec:32:9636897231212746. PMID: 38006220 -
Am J Physiol Endocrinol Metab
Amelioration of bone fragility by pulsed electromagnetic fields in type 2 diabetic KK-Ay mice involving Wnt/β-catenin signaling. [Abstract]2021 May 1;320(5):E951-E966. PMID: 33719588 -
Npj Viruses
The Wnt/β-catenin pathway is important for replication of SARS-CoV-2 and other pathogenic RNA viruses. [Abstract]2024 Feb 21;2(1):6. PMID: 40295745 -
ETC-159 purchased from MedChemExpress. Usage Cited in: PRACTICAL ONCOLOGY JOURNAL. 2018,32(02):103-106.
Effects of ETC-159 on the Wnt signaling pathway in SCC-15 cells.
Solvent & Solubility
DMSO : 50 mg/mL (127.75 mM; Need ultrasonic; 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
HEK293 cells stably transfected with STF reporter and pPGK-WNT3A plasmid (STF3A cells) are treated with varying concentrations of compounds. For Wnt secretion, STF3A cells are treated with ETC-159 diluted in 1% fetal bovine serum-containing media[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: For human xenograft models, patient-derived solid tissue fragments are subcutaneously implanted in BALB/c nude mice. All groups are matched for tumor size with equal variance before treatment. ETC-159 formulated in 50% PEG400 (vol/vol) in water is administered by oral gavage at a dosing volume of 10 μL/g body weight[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
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 | 2.5551 mL | 12.7753 mL | 25.5506 mL | 63.8765 mL |
| 5 mM | 0.5110 mL | 2.5551 mL | 5.1101 mL | 12.7753 mL | |
| 10 mM | 0.2555 mL | 1.2775 mL | 2.5551 mL | 6.3877 mL | |
| 15 mM | 0.1703 mL | 0.8517 mL | 1.7034 mL | 4.2584 mL | |
| 20 mM | 0.1278 mL | 0.6388 mL | 1.2775 mL | 3.1938 mL | |
| 25 mM | 0.1022 mL | 0.5110 mL | 1.0220 mL | 2.5551 mL | |
| 30 mM | 0.0852 mL | 0.4258 mL | 0.8517 mL | 2.1292 mL | |
| 40 mM | 0.0639 mL | 0.3194 mL | 0.6388 mL | 1.5969 mL | |
| 50 mM | 0.0511 mL | 0.2555 mL | 0.5110 mL | 1.2775 mL | |
| 60 mM | 0.0426 mL | 0.2129 mL | 0.4258 mL | 1.0646 mL | |
| 80 mM | 0.0319 mL | 0.1597 mL | 0.3194 mL | 0.7985 mL | |
| 100 mM | 0.0256 mL | 0.1278 mL | 0.2555 mL | 0.6388 mL |
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