Synonyms: BC 1215 | BC1215
Compound class:
Synthetic organic
Comment: BC-1215 has been reported as an inhibitor of cytokine release that acts by targeting the ApaG motif in the C-terminal domain of ubiquitin E3 ligase F box component (Fbxo3) [2-4]. It blocks Fbxo3 interaction with the TRAF inhibitory protein Fbxl2, which results in elevation of Fbxl2-mediated degradation of TRAF proteins and ultimately decreases release of pro-inflammatory cytokines from monocytes. BC-1215 maps to compound 005 in patent US20180071232A, in which it is claimed for potential to treat inflammatory respiratory disease or injury [1].
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. ✖ |
|
References |
1. Chen B, Mallampalli R. (2018)
Compositions and methods for treating respiratory injury or disease. Patent number: US20180071232A. Assignee: University of Pittsburgh , US Department of Veterans Affairs VA. Priority date: 17/11/2017. Publication date: 15/03/2018. |
2. Hung KY, Liao WI, Pao HP, Wu SY, Huang KL, Chu SJ. (2019)
Targeting F-Box Protein Fbxo3 Attenuates Lung Injury Induced by Ischemia-Reperfusion in Rats. Front Pharmacol, 10: 583. [PMID:31178737] |
3. Jeon S, Kang J, Lee SB. (2023)
BC-1215 inhibits ATP-induced IL-1β secretion via the FBXL2-mediated ubiquitination and degradation of not only NLRP3, but also pro-IL-1β in LPS-primed THP-1 cells. Biochem Biophys Res Commun, 657: 128-135. [PMID:37004285] |
4. Mallampalli RK, Coon TA, Glasser JR, Wang C, Dunn SR, Weathington NM, Zhao J, Zou C, Zhao Y, Chen BB. (2013)
Targeting F box protein Fbxo3 to control cytokine-driven inflammation. J Immunol, 191 (10): 5247-55. [PMID:24123678] |