Synonyms: AK2292
Compound class:
Synthetic organic
Comment: AK-2292 is a PROTAC that mediates degradation of the STAT5A/B transcription factors [1]. It contains a STAT5-binding ligand (AK-305; PubChem CID 166594169) linked to lenalidomide moeity that mediates cereblon binding, and directs the STAT5 proteins for ubiquitination and proteosomal degradation. AK-2292 was designed to evaluate STAT5 degradation as a therapeutic strategy for haematologic malignancies such as acute myeloid leukemia (AML). The PROTAC selectively inhibits phosphorylation and transcriptional activity of STAT5 in vitro and in vivo.
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 |
Ligand families/groups | PROTACs, molecular glues and other degraders |
Synonyms |
AK2292 |
Database Links | |
GtoPdb PubChem SID | 479821200 |
PubChem CID | 166594150 |
Search Google for chemical match using the InChIKey | LOPYPDQOHNOVBM-QOIUHGAOSA-N |
Search Google for chemicals with the same backbone | LOPYPDQOHNOVBM |
UniChem Compound Search for chemical match using the InChIKey | LOPYPDQOHNOVBM-QOIUHGAOSA-N |
UniChem Connectivity Search for chemical match using the InChIKey | LOPYPDQOHNOVBM-QOIUHGAOSA-N |