(R)-PFI-2

SAM uncompetitive inhibitor, Peptide competitive inhibitor (in the presence of SAM) of SETD7

Structure

Information

Protein target names: SETD7

Mechanism of action: SAM uncompetitive inhibitor, Peptide competitive inhibitor (in the presence of SAM)

Recommended in-cell concentration:
100 nM - 5 uM

In Vitro Validations

Uniprot ID: Q8WTS6
Target Class: Epigenetic
Target SubClass: Protein methyltransferase
Potency: Ki (app)
Potency Value: 0.33 nM
Potency Assay: IC50 = 2 nM in radioactive methyltransferase assay, transfer of 3H from 3H-SAM to peptide substrate
PDB ID for probe-target interaction (3D structure): 4JLG
Target aliases:
Histone-lysine N-methyltransferase SETD7, SET9, SE ...

DOI Reference: 10.1073/pnas.1407358111

In Cell Validations

In Vivo Data

No in Vivo Validations

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SERP ratings and comments


SERP Ratings

In Cell Rating

(last updated: 17 May 2016 )

SERP Ratings

In Cell Rating

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

In Cell Rating

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 )