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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

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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

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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 public 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