1. NF-κB Cell Cycle/DNA Damage Autophagy Apoptosis
  2. IKK Deubiquitinase Autophagy Apoptosis NF-κB
  3. BAY 11-7082

BAY 11-7082  (Synonyms: BAY 11-7821)

Cat. No.: HY-13453 Purity: 99.89%
COA Handling Instructions

BAY 11-7082 est un inhibiteur de phosphorylation IκBα et NF-κB. BAY 11-7082 inhibe de manière sélective et irréversible la phosphorylation induite par le TNF-α de IκB-α, et diminue NF-κB et l'expression des molécules d'adhésion. BAY 11-7082 inhibe la protéase spécifique à l'ubiquitine USP7 et USP21 (IC50=0,19, 0,96 μM, respectivement). BAY 11-7082 inhibe la gasdermine D (GSDMD) la formation de pores dans les liposomes et la pyroptose induite par les inflammasomes et la sécrétion d'IL-1β dans les cellules humaines et de souris.

BAY 11-7082 ist ein IκBα phosphorylation- und NF-κB-Inhibitor. BAY 11-7082 hemmt selektiv und irreversibel die TNF-α-induzierte Phosphorylierung von IκB-α und verringert NF-κB und die Expression von Adhäsionsmolekülen. BAY 11-7082 hemmt die Ubiquitin-spezifische Protease USP7 und USP21 (IC50=0.19 bzw. 0,96 μM). BAY 11-7082 hemmt die Porenbildung von gasdermin D (GSDMD) in Liposomen und die Sekretion von inflammasomvermittelter Pyroptose und IL-1β in menschlichen und Mauszellen.

BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells.

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

BAY 11-7082 Chemical Structure

BAY 11-7082 Chemical Structure

CAS No. : 19542-67-7

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Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
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USD 61 In-stock
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10 mM * 1 mL in DMSO USD 61 In-stock
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5 mg USD 55 In-stock
10 mg USD 66 In-stock
50 mg USD 231 In-stock
100 mg USD 374 In-stock
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Customer Review

Based on 282 publication(s) in Google Scholar

Top Publications Citing Use of Products

264 Publications Citing Use of MCE BAY 11-7082

WB
RT-PCR

    BAY 11-7082 purchased from MedChemExpress. Usage Cited in: J Cell Biochem. 2019 Mar;120(3):3898-3910.  [Abstract]

    Cells pretreated with SP600125 show a decreased proapoptotic Bax expression and increase antiapoptotic Bcl-2 formation when JNK pathway is blocked. Inhibition of p38 by SB202190 significantly enhanced Bcl-2 expression. Pretreatment with BAY 11-7082 to inhibit NF‐κB markedly enhance Baxm and decrease Bcl-2 expression compared with the ACR-treated group.

    BAY 11-7082 purchased from MedChemExpress. Usage Cited in: BMC Cancer. 2019 Jan 8;19(1):30.  [Abstract]

    The representative images and analysis of western blot for IκBα、p-IκBα and nuclear p65 in CRC cells and expression levels of E-cadherin, N-cadherin and fibronectin in SW620 and HCT116 cells are measured by western blot treated with BAY 11-7082 (inhibitor of NF-κB pathway).

    BAY 11-7082 purchased from MedChemExpress. Usage Cited in: Evid-Based Compl ALlt. 2019 Jan 13;2019:9406342.  [Abstract]

    Protein expressions of AQP3, COX-2 and p-P65 are analyzed by western blot analysis with or without the treatment of BAY and RFP.

    BAY 11-7082 purchased from MedChemExpress. Usage Cited in: Evid-Based Compl ALlt. 2019 Jan 13;2019:9406342.  [Abstract]

    The expressions of p-p65, COX-2 and AQP3 are detected by western blotting with or without the treatment of BAY and RFP.

    BAY 11-7082 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2018 Aug 1;428:77-89.  [Abstract]

    Western blots show that the NF-κB inhibitors BAY11-7082, Parthenolide, and JSH-23 cause dramatic time- and dose-dependent reductions in MGMT protein expression in LN18 and T98G glioma cells.

    BAY 11-7082 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2018 Oct 19;15(1):291.  [Abstract]

    Real-time PCR analysis shows that meningitic E. coli strains PCN033- and RS218-induced proinflammatory cytokines production is significantly decreased via NF-κB signaling inhibition with 10 μM of BAY11-7082.

    BAY 11-7082 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2018 Oct 19;15(1):291.  [Abstract]

    Real-time PCR analysis shows that meningitic E. coli strains PCN033- and RS218-induced proinflammatory cytokines production is significantly decreased via NF-κB signaling inhibition with 10 μM of BAY11-7082.

    BAY 11-7082 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Aug 29;9(9):880.  [Abstract]

    NF-κB inhibitor Bay 11-7082 treatment inhibits the activation of SOX4 and EMT process induced by CXCL1.

    BAY 11-7082 purchased from MedChemExpress. Usage Cited in: Cell Mol Life Sci. 2018 Mar;75(6):1117-1132.  [Abstract]

    Sertoli cells (SC) are pretreated with BAY11-7082 at 2 μM for 1 h, followed by the addition of MC-LR into the culture medium. Expression of p-p65 and MMP-8 is measured by western blotting.

    BAY 11-7082 purchased from MedChemExpress. Usage Cited in: Cell Mol Life Sci. 2018 Jul;75(14):2627-2641.  [Abstract]

    RAW264.7 macrophages are pre-treated with the inhibitor of ERK, JNK, P38, P65, and AKT signal pathway.Western blot analyzes the non- and phosphorylation of ERK, JNK, P38, P65, and AKT.

    BAY 11-7082 purchased from MedChemExpress. Usage Cited in: Front Immunol. 2018 Sep 19;9:2121.  [Abstract]

    RPMI 2650 cells is incubated with or without IL-17A (100 ng/mL)+BAY 11-7082 (5 μM) for 24 h. WB is performed to measure the expression of MMP-9 protein levels.

    BAY 11-7082 purchased from MedChemExpress. Usage Cited in: Lab Invest. 2018 Apr;98(4):462-476.  [Abstract]

    Caco-2BBe cells are pretreated with BAY-11-7082 for 30 min and then treated with TNF-α (100 ng/mL) for 6 h. BAY-11-7082 treatment prevented the TNF-α-induced decrease in downregulated in adenoma (DRA).

    BAY 11-7082 purchased from MedChemExpress. Usage Cited in: Cancer Biol Ther. 2018 Mar 4;19(3):222-229.  [Abstract]

    Western blot analysis of PIK3R3, TP, p-P65, P65 expression after transfected with PIK3R3 at the presence of BAY11-7082.

    BAY 11-7082 purchased from MedChemExpress. Usage Cited in: Environ Pollut. 2017 Oct;229:964-975.  [Abstract]

    NF-κB-dependent immune responses in testicular cells. Sertoli cells (SC), Leydig cells (LC), and germ cells (GC) are pretreated with BAY11-7082 (BAY) at 2 μM for 1 h, followed by the addition of MC-LR into the culture medium to a final concentration of 1 μM and incubation for 6 h. Expression of phosphorylated NF-κB p65 (p-p65) and total p65 is measured by western blotting. The ratio of p-65/p65 is determined by densitometry and is expressed as means±SEM (n=5).

    BAY 11-7082 purchased from MedChemExpress. Usage Cited in: Eur J Med Chem. 2017 Oct 20;139:337-348.  [Abstract]

    The cells are treated with different concentrations of compound 6k, and then in the presence or absence of LPS (1 μg/mL) for 24 h. Bay 11-7082 is the NF-κB inhibitors (20 μM). The results are showed as means±SD (n=3) of at least three independent experiments.

    BAY 11-7082 purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2017 Sep;50:30-37.  [Abstract]

    BV-2 cells are pretreated with or without Bay11-7082 (10 μM) for 30 min, and then incubated with 20 μM Aβ1–42 for 24 h. The protein expression of TNF-α, IL-1β, and IL-6 are detected by western blot.

    BAY 11-7082 purchased from MedChemExpress. Usage Cited in: Toxicol Appl Pharmacol. 2017 Mar 22;323:44-52.  [Abstract]

    The HUVECs are subjected to NF-κB inhibitor BAY 11-7082 (10 μM) for 1 h prior to MGO (1.0 mM) treatment for 24 h, then Bcl-2/ Bax ratio are determined by western blot.

    BAY 11-7082 purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2016 Oct;39:149-57.  [Abstract]

    AOPPs-induced increase in catabolic factors is regulated by NF-κB activation. Chondrocytes are pretreated with or without NF-κB specific inhibitor Bay11-7082 (0.5 μM), followed by AOPPs treatment. NF-κ B p65 phosphorylation, IκB-α degradation and catabolic factors are detected by Western blot analysis. GAG production is determined by DMB method. Addition of Bay11-7082 blocks AOPPs-induced phosphorylation of NF-κB p65 and prevents degradation of IκB-α.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells[1][2][3][4][5].

    IC50 & Target[1][2]

    NF-κB

     

    USP7

    0.19 μM (IC50)

    USP21

    0.96 μM (IC50)

    Autophagy

     

    In Vitro

    BAY 11-7082 (BAY 11-7821), an inhibitor of NF-κB, induces apoptosis of HTLV-I-infected T-cell lines but only negligible apoptosis of HTLV-I-negative T cells. Bay 11-7082 rapidly and efficiently reduces the DNA binding of NF-κB in HTLV-I-infected T-cell lines and down-regulated the expression of the antiapoptotic gene, Bcl-xL, regulated by NF-κB. Bay 11-7082 selectively inhibits Tax-induced NF-κB activity in a human T-cell line[1].
    BAY 11-7082 inhibits NFκB signalling and is recently shown to inhibit the majority of E2 and E3 ligases tested by reacting covalently with the catalytic cysteine residues. Moreover, BAY 11-7082 also inhibits several tyrosine phosphatases by reacting with catalytic Cys residue of these enzymes. NSC 697923 is originally shown to inhibit the E2 ligase Ubc13-Uev1A[2].
    BAY 11-7082 inhibits the phosphorylation of IκBα and activation of NF-κB, induces the death of HBL-1 cells. BAY 11-7082 completely suppresses the LPS-stimulated and IL-1-stimulated phosphorylation of the activation loop of IKKβ[3].
    BAY 11-7082 acts by inhibiting TNF-α-induced phosphorylation of IκB-α, resulting in decreased NF-κB and decreases expression of adhesion molecules[4].

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

    In Vivo

    BAY 11-7082 (2.5 mg/kg and 5 mg/kg; intratumoral injection; twice-weekly for 21 days ) significantly suppresses tumor growth in a dose-dependent manner[6].

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

    Animal Model: Four-week-old male BALB/c nude mice with human gastric carcinoma cell lines HGC-27[6]
    Dosage: Low-dose (2.5 mg/kg body weight), high-dose (5 mg/kg body weight)
    Administration: Intratumoral injection; twice-weekly for 21 days
    Result: Suppressed tumor growth in a dose-dependent manner.
    Molecular Weight

    207.25

    Formula

    C10H9NO2S

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    N#C/C=C/S(=O)(C1=CC=C(C)C=C1)=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 : ≥ 100 mg/mL (482.51 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 4.8251 mL 24.1255 mL 48.2509 mL
    5 mM 0.9650 mL 4.8251 mL 9.6502 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

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

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

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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 (12.06 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.
    • Protocol 2

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

      Solubility: ≥ 2.5 mg/mL (12.06 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    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

    Purity: 99.98%

    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 4.8251 mL 24.1255 mL 48.2509 mL 120.6273 mL
    5 mM 0.9650 mL 4.8251 mL 9.6502 mL 24.1255 mL
    10 mM 0.4825 mL 2.4125 mL 4.8251 mL 12.0627 mL
    15 mM 0.3217 mL 1.6084 mL 3.2167 mL 8.0418 mL
    20 mM 0.2413 mL 1.2063 mL 2.4125 mL 6.0314 mL
    25 mM 0.1930 mL 0.9650 mL 1.9300 mL 4.8251 mL
    30 mM 0.1608 mL 0.8042 mL 1.6084 mL 4.0209 mL
    40 mM 0.1206 mL 0.6031 mL 1.2063 mL 3.0157 mL
    50 mM 0.0965 mL 0.4825 mL 0.9650 mL 2.4125 mL
    60 mM 0.0804 mL 0.4021 mL 0.8042 mL 2.0105 mL
    80 mM 0.0603 mL 0.3016 mL 0.6031 mL 1.5078 mL
    100 mM 0.0483 mL 0.2413 mL 0.4825 mL 1.2063 mL
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      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:
    BAY 11-7082
    Cat. No.:
    HY-13453
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