PFI-1

Antagonist of BRD2, BRD4, BRD3, BRDT

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(2 ratings)

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.

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Information

Protein target names: BRD2, BRD4, BRD3, BRDT

Mechanism of action: Antagonist

Recommended in-cell concentration:

100 nM - 10 uM

Primary References:

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

Probe Availability:

In Vitro Validations

Uniprot ID: P25440

Target Class:

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:

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

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

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

Comments:

This probe meets SGC probe criteria.

(last updated: 22 Jun 2016 )

SERP Ratings

In Cell Rating

(last updated: 3 Jan 2017 )