Bay 11-7821 (BAY 11-7082)

Bay 11-7821 (BAY 11-7082)

Catalog Number:
L002369092APE
Mfr. No.:
APE-A4210
Price:
$196
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      • Overview
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          Background

          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].

          [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.

      • Properties
        • Alternative Name
          (E)-3-(4-methylphenyl)sulfonylprop-2-enenitrile
          CAS Number
          19542-67-7
          Molecular Formula
          C10H9NO2S
          Molecular Weight
          207.25
          Purity
          98.00%
          Solubility
          insoluble in H2O; ≥64 mg/mL in DMSO; ≥10.64 mg/mL in EtOH with gentle warming and ultrasonic
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 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.

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