BAY 11-7082

Catalog No.S2913 Batch:S291303

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Technical Data

Formula

C10H9NO2S

Molecular Weight 207.25 CAS No. 19542-67-7
Solubility (25°C)* In vitro DMSO 41 mg/mL (197.82 mM)
Ethanol 10 mg/mL (48.25 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description BAY 11-7082 (BAY 11-7821) is a NF-κB inhibitor, inhibits TNFα-induced IκBα phosphorylation with IC50 of 10 μM in tumor cells. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 with IC50 of 0.19 μM and 0.96 μM, respectively. BAY 11-7082 induces apoptosis and S phase arrest in gastric cancer cells.
Targets
E2-conjugating enzymes [6]
(Cell-free assay)
USP7 [7]
(Cell-free assay)
USP21 [7]
(Cell-free assay)
USP6 [7]
(Cell-free assay)
IκBα phosphorylation [1]
(Tumor cells)
0.19 μM 0.96 μM 1.7 μM 10 μM
In vitro

BAY 11-7082 completely and specifically abrogates NF-κB DNA binding, downregulating the NF-κB-inducible cytokine IL-6 and inducing apoptosis. [1]

BAY 11-7082 (< 8 μM) is able to effectively inhibit both basal and TNFα stimulated NFκB luciferase activity in a dose dependent manner. BAY 11-7082 (8 μM) strongly inhibits the rate of proliferation in NCI-H1703 cells. [2]

Bay 11-7082 (5 μM) rapidly and efficiently reduces the DNA binding of NF-kappaB in HTLV-I-infected T-cell lines and down-regulates the expression of the antiapoptotic gene, Bcl-x(L), whereas it has little effect on the DNA binding of another transcription factor, AP-1. Bay 11-7082-induced apoptosis of primary ATL cells is more prominent than that of normal peripheral blood mononuclear cells, and apoptosis of these cells is also associated with down-regulation of NF-kappaB activity. Bay 11-7082 (5 μM) selectively induces apoptosis of HTLV-I–infected T-cell lines associated with down-regulation of the expression of cyclin D1, cyclin D2, and Bcl-xL. [3]

BAY 11-7082 (100 μM) prevents the nuclear translocation of p65 elicited by NMDA and the NMDA-induced increase of NF-κB binding in mouse hippocampal slices. BAY 11-7082 prevents NMDA toxicity occurring in CA1 region of hippocampal slices with 40% neuroprotection at 20 μM and 70% neuroprotection at 100 μM. [4]

BAY 11-7082 at all concentrations tested significantly inhibits NF-κB p65 DNA-binding activity in adipose tissue, whereas in skeletal muscle, BAY 11-7082 at 50 μM and 100 μM significantly inhibits NF-κB p65 DNA-binding activity. BAY 11-7082 (100 μM) reduces IKK-β protein in human adipose tissue and skeletal muscle. BAY 11-7082 (100 μM) significantly decreases the release of TNF-α from adipose tissue, whereas the release of IL-6 and IL-8 is significantly inhibited at all concentrations of BAY 11-7082 tested. BAY 11-7082 (50 μM) significantly decreases the release of TNF-α, IL-6, and IL-8 in skeletal muscle. [5]

BAY 11-7082 is also found to inactivate the E2-conjugating enzymes Ubc (ubiquitin conjugating) 13 and UbcH7 and the E3 ligase LUBAC (linear ubiquitin assembly complex), and thus induces B-cell lymphoma and leukaemic T-cell death. [6]

In vivo

BAY 11-7082, an NF-κB inhibitor, induces apoptosis and S phase arrest in gastric cancer cells.

Protocol (from reference)

Cell Assay:

[2]

  • Cell lines

    NCI-H1703 cells

  • Concentrations

    ~8 μM

  • Incubation Time

    12 hours

  • Method

    Cells are transfected with siRNA in 96-well microtiter plates and then cultured for 72 hours in complete NSCLC medium, treated with BAY 11-7082 for 12 hours. Cells are incubated with [3H]thymidine for 3 hours. The cells are collected on filters using an automatic cell harvester and radioactivity on the filters is measured by β-scintillation counting.

Animal Study:

[8]

  • Animal Models

    Male BALB/c nude mice

  • Dosages

    2.5 & 5 mg/kg

  • Administration

    i.t.

Customer Product Validation

Data from [Data independently produced by Int J Cancer, 2014, 135(2), 282-94]

Data from [Data independently produced by Cardiovasc Diabetol, 2014, 13, 41]

Data from [J Biol Chem, 2014, 289(30), 21028-21039]

Data from [Data independently produced by , , Cancer Lett, 2016, 378(2):131-41]

Selleck's BAY 11-7082 has been cited by 359 publications

The efficacy of chemotherapy is limited by intratumoral senescent cells expressing PD-L2 [ Nat Cancer, 2024, 10.1038/s43018-023-00712-x] PubMed: 38267628
Macrophage Tim-3 maintains intestinal homeostasis in DSS-induced colitis by suppressing neutrophil necroptosis [ Redox Biol, 2024, 70:103072] PubMed: 38330550
Glucocorticoid activates STAT3 and NF-κB synergistically with inflammatory cytokines to enhance the anti-inflammatory factor TSG6 expression in mesenchymal stem/stromal cells [ Cell Death Dis, 2024, 15(1):70] PubMed: 38238297
In vivo CRISPR knockout screen identifies p47 as a suppressor of HER2+ breast cancer metastasis by regulating NEMO trafficking and autophagy flux [ Cell Rep, 2024, 43(2):113780] PubMed: 38363674
MUC1-C is a target of salinomycin in inducing ferroptosis of cancer stem cells [ Cell Death Discov, 2024, 10(1):9] PubMed: 38182558
Epigenetic activation of secretory phenotypes in senescence by the FOXQ1-SIRT4-GDH signaling [ Cell Death Dis, 2023, 14(7):481] PubMed: 37516739
CDK1 bridges NF-κB and β-catenin signaling in response to H. pylori infection in gastric tumorigenesis [ Cell Rep, 2023, 42(1):112005] PubMed: 36681899
Dynamic interplay between IL-1 and WNT pathways in regulating dermal adipocyte lineage cells during skin development and wound regeneration [ Cell Rep, 2023, 42(6):112647] PubMed: 37330908
Stromal-induced epithelial-mesenchymal transition induces targetable drug resistance in acute lymphoblastic leukemia [ Cell Rep, 2023, 42(7):112804] PubMed: 37453060
Regulation of PD-L1 expression in non-small cell lung cancer by interleukin-1β [ Front Immunol, 2023, 14:1192861] PubMed: 37441079

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.