BAY 11-7082 acts as an inhibitor of IκBα phosphorylation and NF-κB. It selectively and irreversibly suppresses TNF-α-induced phosphorylation of IκB-α, leading to reduced NF-κB activity and expression of adhesion molecules. Furthermore, BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 with IC50 values of 0.19 μM and 0.96 μM, respectively. Additionally, it hampers gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis, as well as IL-1β secretion in both human and mouse cells [1][2][3][4][5].
体内研究
BAY 11-7082 (2.5 mg/kg and 5 mg/kg; intratumoral injection; twice-weekly for 21 days) effectively inhibits tumor growth in a dose-dependent manner [5].
体外研究
BAY 11-7082 (BAY 11-7821), an NF-κB inhibitor, triggers apoptosis in HTLV-I-infected T-cell lines, while causing minimal apoptosis in HTLV-I-negative T cells. It promptly and effectively diminishes the DNA binding of NF-κB in HTLV-I-infected T-cell lines, consequently suppressing the expression of the antiapoptotic gene Bcl-xL, which is regulated by NF-κB. Moreover, BAY 11-7082 selectively inhibits Tax-induced NF-κB activity in a human T-cell line [1].
BAY 11-7082 inhibits NFκB signaling and has recently been demonstrated to inhibit the majority of E2 and E3 ligases tested by covalently reacting with their catalytic cysteine residues. Additionally, BAY 11-7082 also inhibits several tyrosine phosphatases by reacting with the catalytic cysteine residue of these enzymes. NSC 697923 was initially identified as an inhibitor of the E2 ligase Ubc13-Uev1A [2].
BAY 11-7082 suppresses IκBα phosphorylation and NF-κB activation, leading to cell death in HBL-1 cells. It effectively blocks the phosphorylation of the activation loop of IKKβ induced by both LPS and IL-1 [3].
BAY 11-7082 functions by inhibiting the TNF-α-induced phosphorylation of IκB-α, leading to reduced NF-κB activity and decreased expression of adhesion molecules [4].
BAY 11-7082 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
A549
10 µM
Function Assay
12 h
suppresses Dvl-3 induced activation of p65
25156800
A549
10 μM
Function Assay
1 h
inhibits the increase of phospho-IκBα in PA103-infected cultures
24612488
A549
1 μM
Function Assay
48 h
enhances the up-regulation of IκB and subsequent decrease in Bax expression induced by combined stimulation
23900080
A549
1 μM
Apoptosis Assay
48 h
reduces the cell death induced by combined stimulation
23900080
BAY 11-7082 动物研究
Dose
Mice: 10 mg/kg[5] (i.v.); min = 5 mg/kg[6], max = 20 mg/kg[7] (i.p.)
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