AP-1/NF-κB activation inhibitor 1
Based on 3 publication(s) in Google Scholar
AP-1/NF-κB activation inhibitor 1 is a potent AP-1 and NF-κB mediated transcriptional activation inhibitor (IC50=1 μM), without blocking basal transcription driven by the β-actin promoter. AP-1/NF-κB activation inhibitor 1 has a similar inhibitory effect on the production of IL-2 and IL-8 levels in stimulated cells.
For research use only. We do not sell to patients.
- Purity: 98.08%
- CAS No.: 188936-12-1
- Formula: C13H11F3N4O4
- Molecular Weight:344.25
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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 Citing Use of MedChemExpress (MCE) AP-1/NF-κB activation inhibitor 1
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Jurkat | IC50 |
1 μM
Compound: 39
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Inhibition of AP-1-mediated transcriptional activation in human Jurkat cells by luciferase reporter gene assay
Inhibition of AP-1-mediated transcriptional activation in human Jurkat cells by luciferase reporter gene assay
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[PMID: 24831826] |
| Jurkat | IC50 |
1 μM
Compound: 39
|
Inhibition of NF-kappaB-mediated transcriptional activation in human Jurkat cells by luciferase reporter gene assay
Inhibition of NF-kappaB-mediated transcriptional activation in human Jurkat cells by luciferase reporter gene assay
|
[PMID: 24831826] |
| Jurkat | IC50 |
1 μM
Compound: 1
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Inhibition of AP-1 (activator protein-1) mediated transcriptional activation in Jurkat T-cells
Inhibition of AP-1 (activator protein-1) mediated transcriptional activation in Jurkat T-cells
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[PMID: 10937715] |
| Jurkat | IC50 |
1 μM
Compound: 1
|
Inhibition of NF-kB mediated transcriptional activation in Jurkat T-cells
Inhibition of NF-kB mediated transcriptional activation in Jurkat T-cells
|
[PMID: 10937715] |
Chemical Information
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CAS No. 188936-12-1
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Appearance Solid
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Molecular Weight 344.25
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Formula C13H11F3N4O4
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Color Off-white to light yellow
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SMILES
O=C(C1=CN=C(C(F)(F)F)N=C1NN2C(C(C)=CC2=O)=O)OCC
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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 (3)
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Journal Impact Factor
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Most Recent
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Arthritis Res Ther
Sirt3 improves monosodium urate crystal-induced inflammation by suppressing Acod1 expression. [Abstract]2023 Jul 19;25(1):121. PMID: 37468929 -
Int Dent J
The NF-κB Signalling Regulates the Abnormal Functions of Neutrophils in Severe Periodontal Disease. [Abstract]2025 Oct 25;75(6):103973. PMID: 41145025 -
mSphere
TAK1 phosphorylation mediates macozinone (PBTZ169) induced innate immune activation against tuberculosis. [Abstract]2025 Sep 22:e0051325. PMID: 40980904
Solvent & Solubility
DMSO : 250 mg/mL (726.22 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: ≥ 2.08 mg/mL (6.04 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.04 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 | 2.9049 mL | 14.5243 mL | 29.0487 mL | 72.6216 mL |
| 5 mM | 0.5810 mL | 2.9049 mL | 5.8097 mL | 14.5243 mL | |
| 10 mM | 0.2905 mL | 1.4524 mL | 2.9049 mL | 7.2622 mL | |
| 15 mM | 0.1937 mL | 0.9683 mL | 1.9366 mL | 4.8414 mL | |
| 20 mM | 0.1452 mL | 0.7262 mL | 1.4524 mL | 3.6311 mL | |
| 25 mM | 0.1162 mL | 0.5810 mL | 1.1619 mL | 2.9049 mL | |
| 30 mM | 0.0968 mL | 0.4841 mL | 0.9683 mL | 2.4207 mL | |
| 40 mM | 0.0726 mL | 0.3631 mL | 0.7262 mL | 1.8155 mL | |
| 50 mM | 0.0581 mL | 0.2905 mL | 0.5810 mL | 1.4524 mL | |
| 60 mM | 0.0484 mL | 0.2421 mL | 0.4841 mL | 1.2104 mL | |
| 80 mM | 0.0363 mL | 0.1816 mL | 0.3631 mL | 0.9078 mL | |
| 100 mM | 0.0290 mL | 0.1452 mL | 0.2905 mL | 0.7262 mL |