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(R)-PFI-2 | (R)-PFI-2 : inhibitor of SETD7
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
SETD7
  • Ki (app):0.33 nM
  • IC50:submicromolar
Inhibitor
100 nM - 5 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
1000-fold selective compared with 18 other protein methyltransferases and DNMT
Selectivity Assessment Description:
No notable activity against 134 targets (ion channels, GPCRs, or other enzymes) up to 10 uM.

Potency
Cellular
In Vitro

SETD7

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1073/pnas.1407358111

Negative Control Compounds

(S)-PFI-2

Chemical Information

Molecular Formula C23H25F4N3O3S
SMILEs O=C([C@@H](Cc1cccc(C(F)(F)F)c1)NS(=O)(=O)c1cc(F)c2c(c1)CCNC2)N1CCCC1
InChI InChI=1S/C23H25F4N3O3S/c24-20-13-18(12-16-6-7-28-14-19(16)20)34(32,33)29-21(22(31)30-8-1-2-9-30)11-15-4-3-5-17(10-15)23(25,26)27/h3-5,10,12-13,21,28-29H,1-2,6-9,11,14H2/t21-/m1/s1
Molecular weight 499.16 Da
AlogP 0.0
HBond acceptors 6
HBond donors 2
Atoms 59

References

Publications

Cross References

canSARChEMBLBindingDBPDBPubMedPubMed

Vendors

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Expert Reviews

by SERP
(on 17 May 2016 )
Cellular Use Rating
( The reviewer did not leave any comments )
by SERP
(on 18 May 2016 )
Cellular Use Rating
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...
by SERP
(on 6 Jun 2016 )
Cellular Use Rating
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.
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria