Synonyms: (E)-3-tosylacrylonitrile | BAY-117082 | BAY117082
Compound class:
Synthetic organic
Comment: BAY 11-7082 has long been reported as a NF-κB inhibitor, which inhibits TNFα-induced IκBα phosphorylation (IC50 10μM) [4]. However, an alternative report suggests that BAY 11-7082 reduces the activation of IκB kinases by targeting components of the ubiquitin system, and that this is responsible for its anti-inflammatory effects and induction of B-cell lymphoma and leukaemic T-cell death
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011)
Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1039-45. [PMID:22037377] |
2. Chelko SP, Asimaki A, Lowenthal J, Bueno-Beti C, Bedja D, Scalco A, Amat-Alarcon N, Andersen P, Judge DP, Tung L et al.. (2019)
Therapeutic Modulation of the Immune Response in Arrhythmogenic Cardiomyopathy. Circulation, 140 (18): 1491-1505. [PMID:31533459] |
3. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013)
A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem J, 451 (2): 313-28. [PMID:23398362] |
4. Melisi D, Chiao PJ. (2007)
NF-kappa B as a target for cancer therapy. Expert Opin Ther Targets, 11 (2): 133-44. [PMID:17227230] |
5. Strickson S, Campbell DG, Emmerich CH, Knebel A, Plater L, Ritorto MS, Shpiro N, Cohen P. (2013)
The anti-inflammatory drug BAY 11-7082 suppresses the MyD88-dependent signalling network by targeting the ubiquitin system. Biochem J, 451 (3): 427-37. [PMID:23441730] |