Bay 11-7821(BAY 11-7082)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Bay 11-7821（Bay 11-7082）是IKK的抑制剂，其IC50值为10 μM[1]。
Bay 11-7821可抑制TNFα诱导的IκB-α磷酸化，从而抑制NF-κB，进而抑制TNFα诱发的E-选择素、VCAM-1和ICAM-1的表面表达。据报道，Bay 11-7821并不抑制全部TNFα诱导的磷酸化，只选择性地抑制IκB-α的磷酸化[1]。
实验显示，Bay 11-7821在有效抑制IKK的浓度下具有高毒性。在MM细胞中可抑制细胞坏死。此外，Bay 11-7821通过诱导B细胞淋巴瘤和白血病T细胞的死亡，从而具有抗炎作用。据报道，Bay 11-7821可抑制巨噬细胞中的NALP3炎性复合体[2, 3]。
参考文献：
[1] Pierce JW, Schoenleber R, Jesmok G, Best J, Moore SA, Collins T, Gerritsen ME. Novel inhibitors of cytokine-induced IkappaBalpha phosphorylation and endothelial cell adhesion molecule expression show anti-inflammatory effects in vivo. J Biol Chem. 1997 Aug 22;272(34):21096-103.
[2] Rauert-Wunderlich H1, Siegmund D, Maier E, Giner T, Bargou RC, Wajant H, Stühmer T. The IKK inhibitor Bay 11-7082 induces cell death independent from inhibition of activation of NFκB transcription factors. PLoS One. 2013;8(3):e59292.
[3] Strickson S1, Campbell DG, Emmerich CH, Knebel A, Plater L, Ritorto MS, Shpiro N, Cohen P. The anti-inflammatory drug BAY 11-7082 suppresses the MyD88-dependent signalling network by targeting the ubiquitin system. Biochem J. 2013 May 1;451(3):427-37.
- 1. Can Liu, Qiu Peng, et al. " Deficiency of Lactoferrin aggravates lipopolysaccharide-induced acute inflammation via recruitment macrophage in mice." Biometals. 2022 Jun 1;1-14. PMID: 35650365
- 2. Mingze Ma, Fengxian Shi, et al. "TGF-β promote epithelial-mesenchymal transition via NF-κB/NOX4/ROS signal pathway in lung cancer cells." Mol Biol Rep. 2021 Mar;48(3):2365-2375. PMID: 33792826
- 3. Liu Hui-heng, Wang Jun-sheng, et al. "LPS induced PCT production via TLR-4/NF-кB passway: it is the difference of G-/G+ bacteremia rats." Cytokine. 2020 Oct 7;137:155317. PMID: 33039977
- 4. Ma L, Jiang M, et al. "Cigarette and IL-17A synergistically induce bronchial epithelial-mesenchymal transition via activating IL-17R/NF-κB signaling." BMC Pulm Med. 2020;20(1):26. Published 2020 Jan 30. PMID: 32000730
- 5. Zhang X, Yan K, et al. "Cyclooxygenase 2 promotes proliferation and invasion in ovarian cancer cells via the PGE2/NF-κB pathway." Cell Transplant. 2019 Dec 10:963689719890597. PMID: 31822119
- 6. Wang Z, Chen J, et al. "cGAS/STING axis mediates a topoisomerase II inhibitor-induced tumor immunogenicity." J Clin Invest. 2019 Aug 13;130:4850-4862. PMID: 31408442
- 7. MXinwei Feng, Junfeng Lu, et al. "Mycobacterium smegmatis Induces Neurite Outgrowth and Differentiation in an Autophagy-Independent Manner in PC12 and C17.2 Cells." Front. Cell. Infect. Microbiol. 19 June 2018.
| Storage | Store at -20°C |
| M.Wt | 207.25 |
| Cas No. | 19542-67-7 |
| Formula | C10H9NO2S |
| Solubility | insoluble in H2O; ≥64 mg/mL in DMSO; ≥10.64 mg/mL in EtOH with gentle warming and ultrasonic |
| Chemical Name | (E)-3-(4-methylphenyl)sulfonylprop-2-enenitrile |
| SDF | Download SDF |
| Canonical SMILES | CC1=CC=C(C=C1)S(=O)(=O)C=CC#N |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Cell experiment:[1] | |
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Cell lines |
Non-small cell lung cancer cell line NCI-H1703 |
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Reaction Conditions |
0 ~ 8 μM Bay 11-7821 for 12 h incubation |
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Applications |
Bay 11-7821 (< 8 μM) was able to effectively inhibit both basal and TNFα stimulated NF-κB luciferase activity in a dose dependent manner. Bay 11-7821 (8 μM) strongly inhibited the rate of proliferation in NCI-H1703 cells. |
| Animal experiment:[2] | |
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Animal models |
Mice xenografted with human gastric cancer HGC27 cells |
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Dosage form |
2.5 or 5 mg/kg Twice-weekly intratumoral injection of Bay 11-7821, for 21 days |
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Applications |
Treatment of Bay 11-7821 significantly suppressed tumor growth in a dose-dependent manner. Furthermore, Bay 11-7821 dose-dependently induced cellular apoptosis and inhibited proliferation in tumor xenografts. |
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Note |
The technical data provided above is for reference only. |
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References: 1. Gastonguay A, Berg T, Hauser AD, et al. The role of Rac1 in the regulation of NF-κB activity, cell proliferation, and cell migration in non-small cell lung carcinoma. Cancer Biology & Therapy, 2012, 13(8): 647-656. 2. Chen L, Ruan Y, Wang X, et al. BAY 11-7082, a nuclear factor-κB inhibitor, induces apoptosis and S phase arrest in gastric cancer cells. Journal of Gastroenterology, 2014, 49(5): 864-874. |
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| 描述 | Bay 11-7821是E2泛素（Ub）连接酶和NF-κB的抑制剂。 | |||||
| 靶点 | E2 ubiquitin conjugating enzyme | NF-κB | ||||
| IC50 | 10 μM | |||||
质量控制和MSDS
- 批次:
化学结构
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