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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
Vendors
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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 public 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