(R)-PFI-2
SAM uncompetitive inhibitor, Peptide competitive inhibitor (in the presence of SAM) of SETD7
Structure
In Cells
In Model Organisms
Information
Protein target names: SETD7
Mechanism of action: SAM uncompetitive inhibitor, Peptide competitive inhibitor (in the presence of SAM)
In Vitro Validations
DOI Reference: 10.1073/pnas.1407358111
In Cell Validations
In Vivo Data
No in Vivo Validations
Reagent authentication certificate:
SERP ratings and comments
SERP Ratings
(last updated: 17 May 2016 )
SERP Ratings
Comments:
The enantiomer (S)-PFI-2 is 500-fold less active, making it a useful negative control. Note, the probe also has an unusual cofactor-dependent mechanism of action: (R)-PFI-2 binds to SETD7 only in the presence of SAM; inhibition of SETD7 activity by (R)-PFI-2 is unlikely to be purely substrate-competitive in the classical sense.
(last updated: 18 May 2016 )
SERP Ratings
Comments:
This is currently the most potent probe available for this target. The availability of the negative control compound further strengthens the usability of this inhibitor.
(last updated: 6 Jun 2016 )