BAY 11-7082

BAY 11-7082 is a synthetic small molecule inhibitor primarily recognized for its potent anti-inflammatory and pro-apoptotic properties [2, 11]. It was originally identified as an irreversible inhibitor of cytokine-induced IκBα phosphorylation, which prevents the activation and nuclear translocation of the transcription factor NF-κB [5, 11]. Subsequent research has revealed that BAY 11-7082 is a broad-spectrum agent that targets multiple proteins, including the NLRP3 inflammasome, ubiquitin-specific proteases (such as USP7 and USP21), and protein tyrosine phosphatases [2, 4, 6]. Its mechanism involves the covalent modification of active-site cysteine residues through its Michael acceptor moiety [6, 11]. It also inhibits E2 conjugating enzymes and has been shown to suppress the MyD88-dependent signaling network [3, 4]. Due to its ability to induce apoptosis in various cancer cell lines, it has been investigated for its potential anticancer effects [4, 11]. While widely used as a pharmacological tool in laboratory settings to study the NF-κB pathway and inflammasome signaling, its lack of specificity and potential for off-target toxicity have limited its clinical development [3, 8]. Additionally, it has demonstrated antibacterial activity against certain Gram-positive and Gram-negative pathogens [1].

Other names

BAY 11-7821(E)-3-tosylacrylonitrile3-(4-methylphenylsulfonyl)-2-propenenitrile(E)-3-(4-Methylphenylsulfonyl)-2-propenenitrile

Irreversible inhibition of IκBα phosphorylation and NLRP3 ATPase activity via covalent modification of active-site cysteines by its Michael acceptor moiety.