- Guide to PHARMACOLOGY
Synonyms: CHIR 99021 | CHIR-99021 | CHIR99021 | CT-99021 | CT99021
Compound class: Synthetic organic
Comment: Laduviglusib (CHIR-99021) is an ATP-competitive inhibitor of glycogen synthase kinase-3α and β (GSK-3α/β), equipotent at both isozymes . The chemical structure of CHIR-99021 matches that submitted to the WHO for the INN laduviglusib. GSK-3β has been implicated in multiple human disorders, by influencing a number of significant cellular pathways (including insulin signalling and glycogen synthesis, neurotrophic factor signalling, Wnt signalling, neurotransmitter signalling and microtubule dynamics) . CHIR-99021 acts as a functional Wnt pathway activator [2,10].
Zaki syndrome, a rare disorder of embryonic organ development in humans, can arise due to homozygous mutations in the Wnt ligand secretion mediator gene (WLS) . CHIR-99021 has been used in a mouse model of Zaki syndrome to demonstrate that activation of Wnt pathway signalling can partially restore embryonic development .
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|
|International Nonproprietary Names|
|CHIR 99021 | CHIR-99021 | CHIR99021 | CT-99021 | CT99021|
|CAS Registry No.||252917-06-9|
|GtoPdb PubChem SID||249565694|
|RCSB PDB Ligand||65C|
|Search Google for chemical match using the InChIKey||AQGNHMOJWBZFQQ-UHFFFAOYSA-N|
|Search Google for chemicals with the same backbone||AQGNHMOJWBZFQQ|
|Search PubMed clinical trials||laduviglusib|
|Search PubMed titles||laduviglusib|
|Search PubMed titles/abstracts||laduviglusib|
|SynPHARM||81001 (in complex with glycogen synthase kinase 3 beta)|
|UniChem Compound Search for chemical match using the InChIKey||AQGNHMOJWBZFQQ-UHFFFAOYSA-N|
|UniChem Connectivity Search for chemical match using the InChIKey||AQGNHMOJWBZFQQ-UHFFFAOYSA-N|
Product supplier links are provided as a service to assist in identifying commercial suppliers of reagents that are mentioned on the IUPHAR/BPS Guide to PHARMACOLOGY database website, and do not imply their endorsement by NC-IUPHAR.
Links are provided in return for sponsorship, used to fund improvements to this database. The sponsorship account is managed and audited by the University of Edinburgh, a charitable body registered in Scotland, SC005336. If you are interested in sponsoring the database, please contact us.✖
Cat. No. 4423