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.

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NF-κB-IN-1 Chemical Structure

NF-κB-IN-1 Chemical Structure

CAS No. : 1227098-15-8

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 560 In-stock
Solution
10 mM * 1 mL in DMSO USD 560 In-stock
Solid
1 mg USD 228 In-stock
5 mg USD 480 In-stock
10 mg USD 800 In-stock
25 mg USD 1550 In-stock
50 mg USD 2400 In-stock
100 mg USD 3600 In-stock
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Based on 2 publication(s) in Google Scholar

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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]

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.

  • Molarity Calculator

  • Dilution Calculator

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

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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    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.
In Vivo Dissolution Calculator
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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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
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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NF-κB-IN-1 Related Classifications

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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NF-κB-IN-1
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