NF-κB-IN-1
Based on 3 publication(s) in Google Scholar
NF-κB-IN-1, a 4-arylidene crucumin analogue, is a potent NF-κB signaling pathway inhibitor. NF-κB-IN-1 directly inhibits IKK to block NF-κB activation. NF-κB-IN-1 effectively inhibits the viability of lung cancer cells and attenuates the clonogenic activity of A549 cells.
For research use only. We do not sell to patients.
- Purity: 98.37%
- CAS No.: 1227098-15-8
- Formula: C31H30O8
- Molecular Weight:530.57
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) NF-κB-IN-1
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Flow Cytometry
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WB
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WB
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Cell Imaging/Staining
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WB
Biological Activity
IKK[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | GI50 |
0.53 μM
Compound: 17
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Growth inhibition of human A549 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human A549 cells after 48 hrs by sulforhodamine B assay
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[PMID: 21070043] |
| A549 | GI50 |
0.72 μM
Compound: 17
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Growth inhibition of human A549 cells after 72 hrs by alamar blue method
Growth inhibition of human A549 cells after 72 hrs by alamar blue method
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[PMID: 21070043] |
| A549 | IC50 |
1 μM
Compound: 17
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Inhibition of TNF-alpha-induced NFkappaB nuclear translocation in human A549 cells preincubated for 30 mins before TNFalpha challenge and measured 30 post TNFalpha challenge by fluorescence method
Inhibition of TNF-alpha-induced NFkappaB nuclear translocation in human A549 cells preincubated for 30 mins before TNFalpha challenge and measured 30 post TNFalpha challenge by fluorescence method
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[PMID: 21070043] |
| A549 | IC50 |
2.8 μM
Compound: 17
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Inhibition of IKK in human A549 cells assessed as inhibition of TNF-alpha-induced IkappaB phosphorylation preincubated for 30 mins before TNFalpha challenge
Inhibition of IKK in human A549 cells assessed as inhibition of TNF-alpha-induced IkappaB phosphorylation preincubated for 30 mins before TNFalpha challenge
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[PMID: 21070043] |
| NCI-H157 | GI50 |
0.16 μM
Compound: 17
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Growth inhibition of human NCI-H157 cells after 72 hrs by alamar blue method
Growth inhibition of human NCI-H157 cells after 72 hrs by alamar blue method
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[PMID: 21070043] |
| NCI-H1944 | GI50 |
0.07 μM
Compound: 17
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Growth inhibition of human NCI-H1944 cells after 72 hrs by alamar blue method
Growth inhibition of human NCI-H1944 cells after 72 hrs by alamar blue method
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[PMID: 21070043] |
| NCI-H460 | GI50 |
0.13 μM
Compound: 17
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Growth inhibition of human H460 cells after 72 hrs by alamar blue method
Growth inhibition of human H460 cells after 72 hrs by alamar blue method
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[PMID: 21070043] |
NF-κB-IN-1 (compound 17) (0.001-100 μM; 72 h) inhibits the growth of A549, H1944, H460 and H157 cells, with GI50s of 0.72, 0.07, 0.13, and 0.16 μM, respectively[1].
NF-κB-IN-1 (0.5-25 μM; pretreated for 30 min or 4 h) potently blocks the IκB phosphorylation and degradation in A549 cells[1].
NF-κB-IN-1 (0.1-100 μM; pretreated for 30 min) dose-dependently inhibits the TNFα-induced nuclear translocation of NF-κB in A549 cells, with an IC50s of 1.0 μM[1].
NF-κB-IN-1 (0.1-0.4 μM; 9 d) inhibits lung cancer clonogenic activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549, H1944, H460 and H157 cells
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Concentration:0.001, 0.01, 0.1, 1, 10, 100 μM
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Incubation Time:72 hours
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Result:Decreased viability of lung adenocarcinoma cells A549 and H1944, quamous cell carcinoma cells H157, and large cell carcinoma cells H460 in a dose-dependent manner.
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Cell Line:A549 cells
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Concentration:0.5, 1.0, 2.5, 5.0, 10.0, 25.0 μM
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Incubation Time:Pretreated for 30 min or 4 h
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Result:Blocked IκB phosphorylation, with an IC50 of 2.8 μM.
Blocked IκB degradation in a dose-dependent manner.
Chemical Information
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CAS No. 1227098-15-8
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Appearance Solid
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Molecular Weight 530.57
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Formula C31H30O8
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Color Light yellow to yellow
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SMILES
O=C(/C=C/C(C=C1)=CC(OC)=C1OC)/C(C(/C=C/C(C=C2)=CC(OC)=C2OC)=O)=C/C(C=C3)=CC(OC)=C3O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Cell Commun Signal
Neutrophil extracellular traps induced by the hypoxic microenvironment in gastric cancer augment tumour growth. [Abstract]2023 May 1;21(1):86. PMID: 37127629
NF-κB-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2023 May 1;21(1):86. [Abstract]
Neutrophils were pretreated with inhibitors of the ERK (HY-112287;ERK1/2 inhibitor 1), p38 MAPK (HY-12839; p38 MAPK-IN-1), and p65 NF-кB (HY-138537; NF-κB-IN-1) pathways prior to incubation with hypoxic-CM from GC cells. The protein levels of p-ERK, p-p38, and p-p65 in neutrophils were measured by western blotting.
NF-κB-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2023 May 1;21(1):86. [Abstract]
Neutrophils were pretreated with inhibitors of the ERK (HY-112287;ERK1/2 inhibitor 1), p38 MAPK (HY-12839; p38 MAPK-IN-1), and p65 NF-кB (HY-138537; NF-κB-IN-1) pathways prior to incubation with hypoxic-CM from GC cells. The NET formation by neutrophils was evaluated with MPO and citH3 staining. Magnification: 20 × . Scale bars: 50 μm.
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Cancer Med
Inhibition of FGFR3 upregulates MHC-I and PD-L1 via TLR3/NF-kB pathway in muscle-invasive bladder cancer. [Abstract]2023 Jul;12(14):15676-15690. PMID: 37283287
NF-κB-IN-1 purchased from MedChemExpress. Usage Cited in: Cancer Med. 2023 Jul;12(14):15676-15690. [Abstract]
IKK‐inhibitor (HY‐138537; NF-κB-IN-1) could block NF‐kB activation and decrease the downstream proteins HLA‐A/B/C and PD‐L1.
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Adv Biol (Weinh)
HMGB1 Derived from the Pyroptotic Microenvironment Promotes Macrophage Extracellular Traps in Hirschsprung-Associated Enterocolitis. [Abstract]2025 Jun 4:e00761. PMID: 40464207
NF-κB-IN-1 purchased from MedChemExpress. Usage Cited in: Adv Biol (Weinh). 2025 Jun 4:e00761. [Abstract]
Macrophages were pretreated with inhibitors of the ERK (HY‐112287; ERK1/2 inhibitor 1), JNK (HY‐12041; SP600125), p38 MAPK (HY‐12839; p38 MAPK-IN-1), and p65 NF‐kB (HY‐138537; NF-κB-IN-1) pathways prior to incubation with pyroptotic‐CM for 4 h.The MET formation by macrophages was evaluated with SYTOX Green staining and detected by flow cytometry.
NF-κB-IN-1 purchased from MedChemExpress. Usage Cited in: Adv Biol (Weinh). 2025 Jun 4:e00761. [Abstract]
Macrophages were pretreated with inhibitors of the ERK (HY‐112287; ERK1/2 inhibitor 1), JNK (HY‐12041; SP600125), p38 MAPK (HY‐12839; p38 MAPK-IN-1), and p65 NF‐kB (HY‐138537; NF-κB-IN-1) pathways prior to incubation with pyroptotic‐CM for 4 h. The p‐p38 and p‐p65 levels in macrophages were measured by western blotting.
Solvent & Solubility
DMSO : 50 mg/mL (94.24 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, 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)
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 (4.71 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.
Purity & Documentation
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Data Sheet (275 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)
- 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, 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 | 1.8848 mL | 9.4238 mL | 18.8477 mL | 47.1191 mL |
| 5 mM | 0.3770 mL | 1.8848 mL | 3.7695 mL | 9.4238 mL | |
| 10 mM | 0.1885 mL | 0.9424 mL | 1.8848 mL | 4.7119 mL | |
| 15 mM | 0.1257 mL | 0.6283 mL | 1.2565 mL | 3.1413 mL | |
| 20 mM | 0.0942 mL | 0.4712 mL | 0.9424 mL | 2.3560 mL | |
| 25 mM | 0.0754 mL | 0.3770 mL | 0.7539 mL | 1.8848 mL | |
| 30 mM | 0.0628 mL | 0.3141 mL | 0.6283 mL | 1.5706 mL | |
| 40 mM | 0.0471 mL | 0.2356 mL | 0.4712 mL | 1.1780 mL | |
| 50 mM | 0.0377 mL | 0.1885 mL | 0.3770 mL | 0.9424 mL | |
| 60 mM | 0.0314 mL | 0.1571 mL | 0.3141 mL | 0.7853 mL | |
| 80 mM | 0.0236 mL | 0.1178 mL | 0.2356 mL | 0.5890 mL |