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Chemical Probes Portal (R)-PFI-2.pdf
(R)-PFI-2

Reagent Authentication Certificate:

Protein target name:
SETD7Mechanism of action:
SAM uncompetitive inhibitorPeptide competitive inhibitor (in the presence of SAM)Recommended Concentration for use in cells:
100 nM - 5 uM
Probe Availability
Probe Information
In vitro validation
Potency:
Ki (app)0.33 nM
Potency assay:
IC50 = 2 nM in radioactive methyltransferase assay, transfer of 3H from 3H-SAM to peptide substratePDB ID for probe-target interaction (3D structure):
4JLGPotency assay (off target):
1000-fold selective compared with 18 other protein methyltransferases and DNMTProbe Selectivity in Vitro:
No notable activity against 134 targets (ion channels, GPCRs, or other enzymes) up to 10 uM.In cell validation
Potency in cells:
IC50submicromolar
Target engagement assay (cells):
CETSA and target pull down with a biotinylated derivative of PFI-2.Toxicity
Cytoxicity assay:
YesNotes on cytotoxicity:
No viability noted in four cells lines (HFF, MCF7, MDA-MB231, U2OS) to 50 uM.