Synonyms: (R)-4e [PMID: 35442672]
Compound class:
Synthetic organic
Comment: (R)-STU104 is a first-in-class molecule that inhibits the interaction between the proteins kinases TAK1 (mitogen-activated protein kinase kinase kinase 7; MAP3K7) and MKK3 (mitogen-activated protein kinase kinase 3; MAP2K3) [1]. These kinases are part of the inflammatory signalling cascade that culminates in TNF-α production. (R)-STU104 binds to MKK3 at a location that disrupts its interaction with the upstream kinase TAK1. This action perturbs MKK3 phosphorylation by TAK1 and inhibits downstream signal propagation. Blocking TAK1-mediated phosphorylation of MKK3 with (R)-STU104 reduces TNF-α in vitro and in mouse models of chronic ulcerative colitis (UC). In the mouse models (R)-STU104 was a more effective UC treatment than the approved UC drug mesalazine (a PPARγ inhibitor). In addition to TNF-α, (R)-STU104 reduced production of several pro-inflammatory cytokines in vivo, including IL-1β, IL-6, and IL-23.
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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Classification | |
Compound class | Synthetic organic |
IUPAC Name |
(3R)-4,6-dimethoxy-3-(4-methoxyphenyl)-2,3-dihydroinden-1-one |
Synonyms |
(R)-4e [PMID: 35442672] |
Database Links | |
GtoPdb PubChem SID | 464244147 |
PubChem CID | 156579934 |
Search Google for chemical match using the InChIKey | OYJBHGSSAJNKJF-CQSZACIVSA-N |
Search Google for chemicals with the same backbone | OYJBHGSSAJNKJF |
UniChem Compound Search for chemical match using the InChIKey | OYJBHGSSAJNKJF-CQSZACIVSA-N |
UniChem Connectivity Search for chemical match using the InChIKey | OYJBHGSSAJNKJF-CQSZACIVSA-N |