PFI-E3H1 A chemical handle for GID4

overview

 

Pfizer in collaboration with the SGC have developed a handle PFI-E3H1 and a PEGylated analogue to show that the handle tolerates a substitution at the exit vector. These findings offers opportunities to synthesize proximity-inducing or degrader modalities. 

A control (PFI-7N) has been made for the related probe PFI-7. We recommend incorporating the features of PFI-7N when designing negative controls for PROTACs with PFI-E3H1. Please also see the tab named 'References'.

 

properties
selectivity profile
in vitro potency
cell based assay data
references
  1. Dominic D.G. Owens et al., A chemical probe to modulate human GID4 Pro/N-degron interactions. https://pubmed.ncbi.nlm.nih.gov/38773330/
  2. Aliakbar K Yazdi et al., Chemical tools for the Gid4 subunit of the human E3 ligase C-terminal to LisH (CTLH) degradation complex. https://pubmed.ncbi.nlm.nih.gov/38516600/

 

pk properties
co-crystal structures
synthetic schemes
materials and methods