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Compound class: Synthetic organic
Comment: GSK-J1 is a catalytic site inhibitor that is somewhat selective for the H3K27me3-specific demethylases KDM6A and 6B (a.k.a. UTX and JMJD3 respectively) . The compund has also been shown to inhibit H3K4me3/me2 catalysed by KDM5 enzymes in vitro .
This is a compound from the Structural Genomics Consortium's (SGC) Epigenetics Probes Collection. It reduces lipopolysaccharide-induced proinflammatory cytokine production by human primary macrophages, a process that depends on both JMJD3 and UTX.
Ligand Activity Visualisation Charts
These 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.✖
|Compound class||Synthetic organic|
|CAS Registry No.||1373422-53-7 (source: Scifinder)|
|GtoPdb PubChem SID||178103606|
|RCSB PDB Ligand||K0I, URY|
|Search Google for chemical match using the InChIKey||AVZCPICCWKMZDT-UHFFFAOYSA-N|
|Search Google for chemicals with the same backbone||AVZCPICCWKMZDT|
|SynPHARM||83291 (in complex with lysine demethylase 5B)|
|UniChem Compound Search for chemical match using the InChIKey||AVZCPICCWKMZDT-UHFFFAOYSA-N|
|UniChem Connectivity Search for chemical match using the InChIKey||AVZCPICCWKMZDT-UHFFFAOYSA-N|
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GSK J1 (links to external site)
Cat. No. 4593