JQ1

Inhibitor of BRD2, BRD4, BRD3, BRDT

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(3 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: Inhibitor

Primary References:

DOI - 10.1038/nature09504

Probe Availability:

In Vitro Validations

Uniprot ID: P25440

Target Class: Epigenetic

Target SubClass: Bromodomain

Potency: Kd

Potency Value: 128 nM

Potency Assay: ITC assay

PDB ID for probe-target interaction (3D structure): 2OSS, 3MXF

Target aliases:

Bromodomain-containing protein 2, RING3, KIAA9001, ...

DOI Reference: 10.1038/nature09504

Uniprot ID: P25440

Target Class: Epigenetic

Target SubClass: Bromodomain

Potency: IC50

Potency Value: 76.9 BD1, 32.6 BD2 nM

Potency Assay: alpha screen

PDB ID for probe-target interaction (3D structure): 3ONI

Target aliases:

Bromodomain-containing protein 2, RING3, KIAA9001, ...

DOI Reference: 10.1038/nature09504

In Cell Validations

In Vivo Data

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 18 May 2016 )

SERP Ratings

In Cell Rating

In Model Organisms

Comments:

JQ1 is very potent probe for the BET family of proteins that can be used in cells.

(last updated: 24 May 2016 )

SERP Ratings

In Cell Rating

In Model Organisms

Comments:

This is an excellent selective cellular probe for the BET family of bromodomains, binding potently to all eight (BD1 and BD2 of BRD2/3/4/T). It has been extensively used in cells as a positive control. Its drawback is its suboptimal in vivo pharmacokinetics (IV t_1/2 0.9 hours: source http://dx.doi.org/10.1038%2Fnature09504), so for in vivo studies, I would recommend using other BET-family bromodomain inhibitors.

(last updated: 30 May 2016 )