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PFI-1

Antagonist of BRD2, BRD4, BRD3, BRDT

Structure

Information

  • BRD2
  • BRD4
  • BRD3
  • BRDT
  • Antagonist
  • 100 nM - 10 uM

In Vitro Validations

Uniprot ID: P25440
Target Class: Epigenetic
Target SubClass: Bromodomain
Potency: Kd
Potency Value: BD1 107.9, BD2 143.9 nM
Potency Assay: ITC assays
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Bromodomain-containing protein 2, RING3, KIAA9001, ...

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

Uniprot ID: P25440
Target Class: Epigenetic
Target SubClass: Bromodomain
Potency: IC50
Potency Value: 98 nM
Potency Assay: alpha screen assay
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Bromodomain-containing protein 2, RING3, KIAA9001, ...

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

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): PFI-1 had negligible activity against 42 bromodomains in thermal shift assays, having the most activity against CBP/EP300, which was too weak to quantify in an IC50 assay, and making PFI-1 >300-fold selective for on-target bromodomains.
Probe Selectivity in Vitro:
PFI-1 had negligible activity against 38 protein kinases, 40 human kinases and 14 human membrane receptors (Cerep).
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SERP ratings and comments

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

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 PBMCs with an IL-6 readout, using RPMI media containing 5% FBS (see PMID: 23095041).

(last updated: 18 May 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

This probe meets SGC probe criteria.

(last updated: 22 Jun 2016 )

SERP Ratings

In Cell Rating

(last updated: 3 Jan 2017 )