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- Bay 11-7821 (BAY 11-7082)
Bay 11-7821 (BAY 11-7082)
Size | Price | Stock | Qty |
---|---|---|---|
10mg | $60.00 | In stock | |
25mg | $120.00 | In stock | |
50mg | $190.00 | In stock | |
100mg | $300.00 | In stock | |
Bay 11-7821 (Bay 11-7082) is an inhibitor of IKK with IC50 value of 10μM [1].
Bay 11-7821 inhibits the TNFα-induced phosphorylation of IκB-α, results in an inhibition of NF-κB. This subsequently causes the inhibition of the TNFα-induced surface expression of E-selectin, VCAM-1, and ICAM-1. It is reported that, Bay 11-7821 does not inhibit entire TNFα-induced phosphorylation but selectively inhibits phosphorylation of IκB-α [1].
Experiments show that Bay 11-7821 is highly toxic at concentrations of effective IKK inhibition. It can induce cell necrosis in MM cells. Additionally, Bay 11-7821 is proved to have an anti-inflammatory ability via inducing death of B-cell lymphoma and leukaemic T-cell. It is also reported to inhibit the NALP3 inflammasome in macrophages [2, 3].
References:
[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. Ying-Ge Wang, Chang Lin, et al. "Overexpression of YKL40, IL-6, IL-8, TNF-α in tonsils and the role of YKL40 in childhood with obstructive sleep apnea syndrome." Sci Rep. 2024 Nov 1;14(1):26283. PMID: 39487152
- 2. Fengjiao Gao, Ming Wei , et al. "The Role and Mechanism of Spinal NF-κB-CXCL1/CXCR2 in Rats with Nucleus Pulposus-induced Radicular Pain." Spine (Phila Pa 1976). 2024 Apr 1;49(7):E87-E99. PMID: 38098294
- 3. Xijia Wang, Yutong Hou, et al. "LncRNA IRAIN overcomes imatinib resistance in chronic myeloid leukemia via NF-κB/CD44 pathway inhibition." iScience. 2024 Apr 30;27(6):109851. PMID: 38784023
- 4. Wenbo Lei, Yating Wen, et al. "Chlamydia trachomatis T3SS Effector CT622 Induces Proinflammatory Cytokines Through TLR2/TLR4-Mediated MAPK/NF-κB Pathways in THP-1 Cells." J Infect Dis. 2023 Dec 26:jiad597. PMID: 38147361
- 5. Paula I Seoane, et al. "Squaramides enhance NLRP3 inflammasome activation by lowering intracellular potassium." Cell Death Discov. 2023 Dec 22;9(1):469. PMID: 38129373
- 6. Xiahong Tang, Jun Ke, et al. "Hypoxic preconditioned mesenchymal stem cells ameliorate rat brain injury after cardiopulmonary resuscitation by suppressing neuronal pyroptosis." J Cell Mol Med. 2023 Jul;27(13):1836-1858. PMID: 37246833
- 7. 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
- 8. 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
- 9. 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
- 10. 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
- 11. 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
- 12. 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
- 13. 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 |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Cell experiment:[1] | |
Cell lines |
Non-small cell lung cancer cell line NCI-H1703 |
Reaction Conditions |
0 ~ 8 μM Bay 11-7821 for 12 h incubation |
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] | |
Animal models |
Mice xenografted with human gastric cancer HGC27 cells |
Dosage form |
2.5 or 5 mg/kg Twice-weekly intratumoral injection of Bay 11-7821, for 21 days |
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. |
Note |
The technical data provided above is for reference only. |
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. |
Description | Bay 11-7821 is an inhibitor of E2 ubiquitin (Ub) conjugating enzyme and NF-κB. | |||||
Targets | E2 ubiquitin conjugating enzyme | NF-κB | ||||
IC50 | 10 μM |
Quality Control & MSDS
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