受注:045-509-1970 |
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Synonyms | BAY 11-7821 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C10H9NO2S |
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分子量 | 207.25 | CAS No. | 19542-67-7 | ||||||||
Solubility (25°C)* | 体外 | DMSO | 41 mg/mL (197.82 mM) | ||||||||
Ethanol | 3 mg/mL (14.47 mM) | ||||||||||
Water | Insoluble | ||||||||||
体内 (毎回新しく調製した物を用意してください) |
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* <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. |
製品説明 | 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. |
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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. |
細胞アッセイ | 細胞株 | NCI-H1703 cells |
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濃度 | ~8 μM | |
反応時間 | 12 hours | |
実験の流れ | 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. |
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動物実験 | 動物モデル | Male BALB/c nude mice |
投薬量 | 2.5 & 5 mg/kg | |
投与方法 | i.t. |
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]
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 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。