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PFI-1 | Antagonist of BRD2, BRD4, BRD3, BRDT
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (2 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
BRD2
  • Kd:BD1 107.9, BD2 143.9 nM
  • IC50:98 nM
BRD4
  • Kd:BD1 47.4 nM, BD2 194.6 nM
  • IC50:220 nM
BRD3
  • Kd:BD1 80 nM, BD2 76.3 nM
BRDT
  • Kd:BD1 85.5, BD2 220 nM
Antagonist
100 nM - 10 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
PFI-1 had negligible activity against 42 bromodomains in thermal shift assays, having the most activ ...
Selectivity Assessment Description:
PFI-1 had negligible activity against 38 protein kinases, 40 human kinases and 14 human membrane rec ...

Potency
Cellular
In Vitro

BRD2

Mode of Action: Antagonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1158/0008-5472.CAN-12-3292

BRD4

Mode of Action: Antagonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1158/0008-5472.CAN-12-3292

BRD3

Mode of Action: Antagonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1158/0008-5472.CAN-12-3292

BRDT

Mode of Action: Antagonist

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1158/0008-5472.CAN-12-3292

Orthogonal Probes def

JQ1
MZ1
CPI-0610

Chemical Information

Molecular Formula C16H17N3O4S
SMILEs COc1ccccc1S(=O)(=O)Nc1ccc2c(c1)CN(C)C(=O)N2
InChI InChI=1S/C16H17N3O4S/c1-19-10-11-9-12(7-8-13(11)17-16(19)20)18-24(21,22)15-6-4-3-5-14(15)23-2/h3-9,18H,10H2,1-2H3,(H,17,20)
Molecular weight 347.09 Da
AlogP 2.4733
HBond acceptors 7
HBond donors 2
Atoms 41

References

Publications

Cross References

GDSC1

Vendors

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

Expert Reviews

by SERP
(on 18 May 2016 )
Cellular Use Rating
In Model Organisms
This probe meets minimal criteria for use in both cellular and in vivo assays. Plasma protein binding information relevant to its use: PFI-1 displayed an IC50 of 1.89 uM (n=6) in LPS-stimulated...
by SERP
(on 22 Jun 2016 )
Cellular Use Rating
In Model Organisms
This probe meets SGC probe criteria.
by SERP
(on 3 Jan 2017 )
Cellular Use Rating
( The reviewer did not leave any comments )
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