PCI-34051
Unsuitables - unsuitable to be used as a chemical probe
Structure
This is unsuitable as a chemical probe: While this
compound has been used to interrogate specific protein
targets, it is not a chemical probe and should not be used
in assays that depend on a potent and selective modulator
of the protein.
Non selective compound
Intended target=HDAC8; Although there is excellent evidence that PCI-34051 is selective for HDAC8 over other HDACs in in vitro biochemical assays, there is scant evidence that this compound acts on target in cells (PMIDs: 18256683, 24380043). There is also good evidence from PET imaging studies, that this molecule does not cross the blood-brain barrier in rodent models (PMID: 24380043). Application of PCI-34051 in cells as a selective HDAC8 inhibitor should be pursued with caution (and with ample control experiments to validate that any observed effects derive from HDAC8-specific activity).