1. NF-κB
  2. IKK
  3. NF-κB-IN-1

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.

CAS No. : 1227098-15-8

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10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

    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.

    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.

    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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    Description

    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[1].

    IC50 & Target

    IKK[1]

    Cellular Effect
    Cell Line Type Value Description References
    A549 GI50
    0.53 μM
    Compound: 17
    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
    [PMID: 21070043]
    A549 GI50
    0.72 μM
    Compound: 17
    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
    [PMID: 21070043]
    A549 IC50
    1 μM
    Compound: 17
    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
    [PMID: 21070043]
    A549 IC50
    2.8 μM
    Compound: 17
    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
    [PMID: 21070043]
    NCI-H157 GI50
    0.16 μM
    Compound: 17
    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
    [PMID: 21070043]
    NCI-H1944 GI50
    0.07 μM
    Compound: 17
    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
    [PMID: 21070043]
    NCI-H460 GI50
    0.13 μM
    Compound: 17
    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
    [PMID: 21070043]
    In Vitro

    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.

    Cell Viability Assay[1]

    Cell Line: A549, H1944, H460 and H157 cells
    Concentration: 0.001, 0.01, 0.1, 1, 10, 100 μM
    Incubation Time: 72 hours
    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.

    Western Blot Analysis[1]

    Cell Line: A549 cells
    Concentration: 0.5, 1.0, 2.5, 5.0, 10.0, 25.0 μM
    Incubation Time: Pretreated for 30 min or 4 h
    Result: Blocked IκB phosphorylation, with an IC50 of 2.8 μM.
    Blocked IκB degradation in a dose-dependent manner.
    Molecular Weight

    530.57

    Formula

    C31H30O8

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    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

    Shipping

    Room temperature in continental US; may vary elsewhere.

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

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8848 mL 9.4238 mL 18.8477 mL
    5 mM 0.3770 mL 1.8848 mL 3.7695 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.

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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    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.
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    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).
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    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
    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
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    • 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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    Product Name:
    NF-κB-IN-1
    Cat. No.:
    HY-138537
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