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BAY 11-7082

CAS号

19542-67-7

分子式

C10H9NO2S

主要靶点

Autophagy|Apoptosis|Others|DUB|IκB/IKK

仅限科研使用

Cat No : CM04718

Print datasheet

Synonyms

IκB|IκB kinase|IκBα?phosphorylation|Inhibitor|inhibit|leukaemic|lymphoma|phosphorylation|T-cell|ubiquitin|Apoptosis|adhesion|BAY 11-7821|BAY 117082|BAY 11-7082|BAY 11 7082|B-cell|Autophagy|Deubiquitinase|cytokine|E2-conjugating enzymes|DUBs|inflammasome|IKK|IkB/IKK|IkB|I kappa B kinase

验证数据展示

  • CAS No.: 19542-67-7

    BAY 11-7082
    CAS#: 19542-67-7

产品信息

CAS号 19542-67-7
分子式 C10H9NO2S
主要靶点 Autophagy|Apoptosis|Others|DUB|IκB/IKK
主要通路 细胞周期|DNA 损伤和修复|泛素化|NF-κB 信号通路|凋亡|自噬
分子量 207.25
纯度 99.92%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 store at low temperature,keep away from direct sunlight,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 IκB|IκB kinase|IκBα?phosphorylation|Inhibitor|inhibit|leukaemic|lymphoma|phosphorylation|T-cell|ubiquitin|Apoptosis|adhesion|BAY 11-7821|BAY 117082|BAY 11-7082|BAY 11 7082|B-cell|Autophagy|Deubiquitinase|cytokine|E2-conjugating enzymes|DUBs|inflammasome|IKK|IkB/IKK|IkB|I kappa B kinase

靶点活性

IκBα?phosphorylation:10 μM

体内活性

方法：为研究免疫调节作用，将 BAY 11-7082 (5-10 mg/kg) 腹腔注射给 C57BL/6 小鼠，1 h 后静脉注射 poly U (50 μg/head) + in vivo-jetPEI。 结果：当 TLR 配体刺激时，用 BAY 11-7082 处理可以通过限制 pDC 功能来抑制体内 IFN 反应。[3] 方法：为研究对银屑病样皮炎的作用，将 BAY 11-7082 (20 mg/kg) 腹腔注射给 IMQ 诱导银屑病样病变的 C57BL/6 和 NLRP3 KO 小鼠，每天一次，持续七天。 结果：BAY 11-7082 钝化表皮厚度、棘皮病和炎症浸润。BAY 11-7082 降低了 pNF-κB、NLRP3、TNF-α、IL-6 和 IL-1β 的表达，减弱了信号转导子和 STAT3 的磷酸化，并降低了 IL-23 水平。[4]

体外活性

方法：人结直肠癌细胞 HT29 用 BAY 11-7082 (10-100 μM) 处理 1 h，随后用 TNF (50 ng/mL) 刺激 3-10 min 或用 Flag-TWEAK (200 ng/mL) 处理 8 h，使用 Western Blot 检测靶点蛋白表达水平。 结果：Bay 11-7082 抑制 TWEAK 诱导的 p100 加工和 TNF 诱导的 IκBα 的磷酸化和降解。在 Bay 11-7082 的浓度为 30-100 μM 时，两种 NFκB 途径均被显著阻断。[1] 方法：巨噬细胞 RAW264.7 用 BAY 11-7082 (15 μM) 和 LPS (1? μg/mL) 处理 6 h，使用 ELISA Assay 检测 TNF-α 水平。 结果：BAY 11-7082 阻断了 LPS 处理的 RAW264.7 细胞中 TNF-α 的产生，这是由活化的 NF-κB 产生的炎症反应。[2]

溶解度

DMSO:60 mg/mL (289.51 mM); Ethanol:5.2 mg/mL (25.09 mM);

细胞实验

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.(Only for Reference)

参考文献

1.Rauert-Wunderlich H, et al. The IKK inhibitor Bay 11-7082 induces cell death independent from inhibition of activation of NFκB transcription factors. PLoS One. 2013;8(3):e59292.
2.Gao J, Wang Y, Zhang W, et al. C20orf27 Promotes Cell Growth and Proliferation of Colorectal Cancer via the TGFβR-TAK1-NF?B Pathway[J]. Cancers. 2020, 12(2): 336.
3.Lee J, et al. BAY 11-7082 is a broad-spectrum inhibitor with anti-inflammatory activity against multiple targets. Mediators Inflamm. 2012;2012:416036.
4.Miyamoto R, et al. Inhibitor of IkappaB kinase activity, BAY 11-7082, interferes with interferon regulatory factor 7 nuclear translocation and type I interferon production by plasmacytoid dendritic cells. Arthritis Res Ther. 2010;12(3):R87.
5.Irrera N, et al. BAY 11-7082 inhibits the NF-κB and NLRP3 inflammasome pathways and protects against IMQ-induced psoriasis. Clin Sci (Lond). 2017 Mar 1;131(6):487-498.
6.Goffi F, et al. Neurosci Lett, 2005, 377(3), 147-151.
7.Jun Jacob Hu, et al. Identification of pyroptosis inhibitors that target a reactive cysteine in gasdermin D. The Preprint Server For Biology, 2018,Jul. 10.
8.Shen S C, He F, Cheng C, et al. Uric acid aggravates myocardial ischemia–reperfusion injury via ROS/NLRP3 pyroptosis pathway[J]. Biomedicine & Pharmacotherapy . 2020, 133: 110990.
9.Yu Y, Li Z, Guo R, et al. Ononin, sec-O-β-D-glucosylhamaudol and astragaloside I: antiviral lead compounds identified via high throughput screening and biological validation from traditional Chinese medicine Zhongjing formulary[J]. Pharmacological Research. 2019 May 11;145:104248.

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