BAY 11-7082 - Moligand™, 10mM in DMSO , CAS No.19542-67-7

CAS: 19542-67-7 Cat. No.: B408448 Peso molecular: 207.25 Número EC: 805-917-7

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

BAY 11-7821 | 2-Propenenitrile, 3-[(4-methylphenyl)sulfonyl]-, (2E)-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

BAY 11-7082 (BAY 11-7821) is aNF-κBinhibitor, inhibits TNFα-inducedIκBαphosphorylation withIC50of 10 μM in tumor cells. BAY 11-7082 inhibitsubiquitin-specific protease USP7andUSP21with IC50 of 0.19 μM and 0.96 μM, respectively. BAY 11-7082 inducesapoptosi
In vitro

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

Cell Data

cell lines：

Concentrations：~8 μM

Incubation Time：12 hours

Powder Purity:≥99%

Specifications

Sinónimos

BAY 11-7821 | 2-Propenenitrile, 3-[(4-methylphenyl)sulfonyl]-, (2E)-

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

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 induc

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Nombres e identificadores

• Isómeros SMILES: CC1=CC=C(C=C1)S(=O)(=O)/C=C/C#N
• WGK Alemania: 3
• Peso molecular: 207.25
• Reaxy-Rn: 2049370
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=2049370&ln=

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: 100 mg/mL (528.48 mM); Water: 100 mg/mL warmed with 50ºC Water: bath (528.48 mM); Ethanol: 100 mg/mL (528.48 mM)
• Punto de fusión (°C): 134℃

Referencias

1. Yu Zhong, Ouyang Ling.  (2023)  OSR1 downregulation indicates an unfavorable prognosis and activates the NF-κB pathway in ovarian cancer.  Discover Oncology,  14  (1): (1-14).  [PMID:37642735] [10.1007/s12672-023-00778-0]

2. Wen Weijia, Li Jiaying, Yuan Li, Liao Yan, Shao Caixia, Xu Dingze, Jiang Hongye, Liao Yuandong, Liu Pan, Zhang Chunyu, Yao Shuzhong, Wang Wei.  (2025)  PRDX3 Promotes Lymph Node Metastasis in Cervical Cancer by Activating NF-κB Signaling Pathway and Anoikis Resistance.  International Journal of Medical Sciences,  22  (15): (3839-3853).  [PMID:41049446] [10.7150/ijms.118912]

3. Shao-Qian Wang, Hui Yuan, Hao-Qiang Qin, Ming-Yue Peng, Ming-Xiao Cui, Ke-Hai Liu.  (2025)  Ultrasonic extraction, Structural Characterization, and Immunoactivity of Polysaccharides From Syzygium jambos (L.) Alston.  CHEMISTRY & BIODIVERSITY,      [PMID:40921029] [10.1002/cbdv.202500537]

4. Yu Shan, Yang Jinghui, Zhang Rui, Guo Qian, Wang Lu.  (2024)  SLC15A3 is transcriptionally regulated by HIF1α and p65 to worsen neuroinflammation in experimental ischemic stroke.  MOLECULAR NEUROBIOLOGY,      [PMID:38717559] [10.1007/s12035-024-04191-8]

5. Ruobing Wang, Dan Su, Yueze Liu, Hua Huang, Jiangdong Qiu, Zhe Cao, Gang Yang, Hao Chen, Wenhao Luo, Jinxin Tao, Guihu Weng, Taiping Zhang.  (2024)  The NF-κB/NUAK2 signaling axis regulates pancreatic cancer progression by targeting SMAD2/3.  iScience,      [PMID:38510132] [10.1016/j.isci.2024.109406]

6. Fang-Fang Liu, Hai-Yan Ren, Feng Liu, Wen-Xuan Qi, Chao-Peng Liang, Bang-Xian Zhang, Xiang-Jun Rao.  (2025)  Time-series RNA sequencing reveals that immulectin-1 (IML-1) is a potential target for biological control of fall armyworm, Spodoptera frugiperda.  INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES,      [PMID:40139608] [10.1016/j.ijbiomac.2025.142466]