1. NF-κB Metabolic Enzyme/Protease
  2. IKK E1/E2/E3 Enzyme NF-κB
  3. GS143

GS143 is a selec­tive IκBα ubiquitination inhibitor with an IC50 of 5.2 μM for SCFβTrCP1-mediated IκBα ubiquitylation. GS143 sup­presses NF-κB acti­va­tion and tran­scrip­tion of tar­get genes and does not inhibit proteasome activity. GS143 has anti-asthma effect.

For research use only. We do not sell to patients.

GS143 Chemical Structure

GS143 Chemical Structure

CAS No. : 916232-21-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 113 In-stock
Solution
10 mM * 1 mL in DMSO USD 113 In-stock
Solid
5 mg USD 110 In-stock
10 mg USD 176 In-stock
25 mg USD 352 In-stock
50 mg USD 550 In-stock
100 mg USD 935 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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  • References

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Description

GS143 is a selec­tive IκBα ubiquitination inhibitor with an IC50 of 5.2 μM for SCFβTrCP1-mediated IκBα ubiquitylation. GS143 sup­presses NF-κB acti­va­tion and tran­scrip­tion of tar­get genes and does not inhibit proteasome activity. GS143 has anti-asthma effect[1][2].

IC50 & Target

IC50: 5.2 μM (SCFβTrCP1-mediated IκBα ubiquitylation)[2]

In Vitro

GS143 (10 μM or 20 μM) inhibits antigen-induced differentiation of Th2 cells but not of Th1 cells in vitro. The IL-4 pro­duc­tion in Th2-polar­iz­ing con­di­tion is mark­edly sup­pressed by GS143 in a dose-depen­dent man­ner[1].
GS143 suppresses the transcription of TNFα-induced NF-κB with a mean IC50 value of 10.5 μM. GS143 also inhibits TNFα-induced expression of ICAM-1 in HT-29 colon cancer cells with an IC50 value of 6.1 μM. The production levels of TNFα and IL-1β in LPS-activated THP-1 cells are inhibited with IC50 values of 5.3 μM and 2.1 μM, respectively. GS143 does not inhibit p53 and β-catenin[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

GS143 (16-32 μg/body; intranasal administration; once; BALB/c mice) treatment suppresses antigen-induced NF-κB activation in the lung of sensitized mice. GS143 treatment also inhibits antigen-induced eosinophil and lymphocyte recruitment into the airways and the expression of Th2 cytokines and eotaxin in the airways[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c mice (age 7-8weeks) injected with oval­bu­min[1]
Dosage: 16 μg/body or 32 μg/body
Administration: Intranasal administration; once
Result: Suppressed antigen-induced NF-κB activation in the lung of sensitized mice.
Molecular Weight

466.46

Formula

C28H19FN2O4

CAS No.
Appearance

Solid

Color

Pink to red

SMILES

FC(C=CC=C1)=C1C2=CC=C(O2)/C=C3C(CC4=CC=CC=C4)=NN(C5=CC=C(C(O)=O)C=C5)C\3=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 37.5 mg/mL (80.39 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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1438 mL 10.7190 mL 21.4381 mL
5 mM 0.4288 mL 2.1438 mL 4.2876 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: 2.08 mg/mL (4.46 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.08 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

  • Protocol 2

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 1.88 mg/mL (4.03 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 1.88 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (18.8 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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+
%
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Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.09%

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, 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 2.1438 mL 10.7190 mL 21.4381 mL 53.5952 mL
5 mM 0.4288 mL 2.1438 mL 4.2876 mL 10.7190 mL
10 mM 0.2144 mL 1.0719 mL 2.1438 mL 5.3595 mL
15 mM 0.1429 mL 0.7146 mL 1.4292 mL 3.5730 mL
20 mM 0.1072 mL 0.5360 mL 1.0719 mL 2.6798 mL
25 mM 0.0858 mL 0.4288 mL 0.8575 mL 2.1438 mL
30 mM 0.0715 mL 0.3573 mL 0.7146 mL 1.7865 mL
40 mM 0.0536 mL 0.2680 mL 0.5360 mL 1.3399 mL
50 mM 0.0429 mL 0.2144 mL 0.4288 mL 1.0719 mL
60 mM 0.0357 mL 0.1787 mL 0.3573 mL 0.8933 mL
80 mM 0.0268 mL 0.1340 mL 0.2680 mL 0.6699 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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GS143
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