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ETC-159

Name: ETC-159
Brand: TargetMol
SKU: T4043
Price: 43 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T4043Cas No. 1638250-96-0

Alias ETC-1922159, ETC159, ETC 159

ETC-159 (ETC-1922159) is a potent, orally available PORCN inhibitor that inhibits β-catenin reporter activity with an IC50 of 2.9 nM.

ETC-159

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Purity: 99.30%

Catalog No. T4043Alias ETC-1922159, ETC159, ETC 159Cas No. 1638250-96-0

ETC-159 (ETC-1922159) is a potent, orally available PORCN inhibitor that inhibits β-catenin reporter activity with an IC50 of 2.9 nM.

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$43	In Stock	In Stock
10 mg	$68	In Stock	In Stock
25 mg	$126	In Stock	In Stock
50 mg	$207	In Stock	In Stock
100 mg	$369	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$48	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.30%

Color:White

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COA HNMR LCMS

Product Introduction

ETC-159 AI Summary

ETC-159 exhibits potent inhibitory activity against porcupine enzymes, demonstrating significant bioactivity across various cell types. Remarkably, it inhibits Wnt secretion by suppressing beta-catenin reporter activity in human HEK293 cells with an IC50 value of 2.9 nM, and shows inhibitory effects on mouse and xenopus porcupine expressed in human HT1080 cells, with IC50 values of 18.1 nM and 70.0 nM, respectively. The compound also displays promising antitumor activity, effectively inhibiting tumor growth by 90.0% in human HPAF2 cells xenografted in Balb/c mice at a dose of 100 mg/kg. Additionally, ETC-159 has exhibited antiviral activity against SARS-CoV-2 in various assays. It inhibited the cytotoxicity of Caco-2 cells at 10 µM after 48 hours with an inhibition rate of -5.76%, and demonstrated inhibitory activity against the SARS-CoV-2 3CL-Pro protease at 20 µM with inhibition percentages of 8.02% and 11.27%. Despite these promising findings, its inhibitory effects varied when tested on VERO-6 cells, showing a range from -0.02% to -0.15%. ETC-159 also inhibits human HDAC6, displaying 41.83% inhibition with a commercial peptide substrate, although showing minimal activity with a custom substrate (-1.95%). The compound is orally bioavailable with 100.0% in mice at a dosage of 10 mg/kg and also exhibits strong antitumor activity against human HEK293 cells xenografted in Sprague-Dawley mice, resulting in a tumor growth inhibition of 94.0% at the same dosage..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	ETC-159 (ETC-1922159) is a potent, orally available PORCN inhibitor that inhibits β-catenin reporter activity with an IC50 of 2.9 nM.
Targets&IC50	β-catenin:2.9 nM.
Synonyms	ETC-1922159, ETC159, ETC 159

Chemical Properties

Molecular Weight	391.38
Formula	C₁₉H₁₇N₇O₃
Cas No.	1638250-96-0
Smiles	Cn1c2ncn(CC(=O)Nc3ccc(nn3)-c3ccccc3)c2c(=O)n(C)c1=O
Relative Density.	1.47 g/cm3 (Predicted)

Storage & Solubility Information

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: 55 mg/mL (140.53 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.11 mM), Sonication is recommended.

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

	1mg	5mg	10mg	50mg
1 mM	2.5551 mL	12.7753 mL	25.5506 mL	127.7531 mL
5 mM	0.5110 mL	2.5551 mL	5.1101 mL	25.5506 mL
10 mM	0.2555 mL	1.2775 mL	2.5551 mL	12.7753 mL
20 mM	0.1278 mL	0.6388 mL	1.2775 mL	6.3877 mL
50 mM	0.0511 mL	0.2555 mL	0.5110 mL	2.5551 mL
100 mM	0.0256 mL	0.1278 mL	0.2555 mL	1.2775 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent 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.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent 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 TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc