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Compound class: Synthetic organic
Comment: THZ1 is a covalent inhibitor of the cyclin-dependent kinase, CDK7 . The compound achieves CDK7 specificity by targeting a remote cysteine residue located outside of the canonical kinase domain. It was a preclinical lead compound.
CDK7 inhibition by THZ1 has been demonstrated to overcome tumour resistance (primary or acquired) to smoothened inhibitor drugs (such as sonidegib, vismodegib and glasdegib), principally via suppressed synthesis of two core transcription factors belonging to the hedgehog pathway (the glioma-associated oncogenes GLI1 and GLI2) . This effect was detected in vitro and in vivo.
CDK7 inhibition has been shown to overcome resistance to HER2-targeted inhibitors in HER2 +ve breast cancer cells and in xenograft models .
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.||1604810-83-4|
|GtoPdb PubChem SID||249565732|
|Search Google for chemical match using the InChIKey||OBJNFLYHUXWUPF-IZZDOVSWSA-N|
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|Search UniChem for chemical match using the InChIKey||OBJNFLYHUXWUPF-IZZDOVSWSA-N|
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