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JQ1

Inhibitor of BRD2, BRD4, BRD3, BRDT

Structure

Information

Protein target names: BRD2, BRD4, BRD3, BRDT

Mechanism of action: Inhibitor

Recommended in-cell concentration:
10 nM - 1 uM
Primary References:

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

SERP 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

SERP 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 t1/2 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 )