Bay 11-7821

A selective and irreversible NF-κB inhibitor

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货号: ajci10312
CAS: 19542-67-7
别名: BAY 11-7082
分子式: C10H9NO2S
分子量: 207.25
纯度: >98%
溶解度: ≥ 64 mg/mL in DMSO, ≥ 10.64 mg/mL in EtOH with ultrasonic and warming
储存: Store at -20°C
库存: 现货

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].

Bay 11-7821（Bay 11-7082）是一种IKK抑制剂，其IC50值为10μM[1]。

Bay 11-7821抑制TNFα诱导的IκB-α磷酸化，导致NF-κB的抑制。这随后导致TNFα诱导的E-selectin、VCAM-1和ICAM-1的表面表达受到抑制。有报道称，Bay 11-7821并不完全抑制TNFα诱导的磷酸化，而是选择性地抑制IκB-α的磷酸化[1]。

实验表明，Bay 11-7821在有效抑制IKK的浓度下具有很高的毒性。它可以在多发性骨髓瘤细胞中诱导细胞坏死。此外，Bay 11-7821被证明具有抗炎能力，可以诱导B细胞淋巴瘤和白血病T细胞的死亡。有报道称它还可以抑制巨噬细胞中的NALP3炎症小体[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.