DN02

DN02 : Inhibitor of BRD8

Structure

SERP Rating

In Cells

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In Model Organisms

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Probe DN02 is in the process of SERP review.

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Information

BRD8

Inhibitor

up to 1 uM

In Vitro Validations

Uniprot ID: Q9H0E9

Target Class: Epigenetic

Target SubClass: Bromodomain

Potency: IC50

Potency Value: 48 nM

Potency Assay: AlphaScreen

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

Target aliases:

Bromodomain-containing protein 8, SMAP2, SMAP, BRD ...

DOI Reference: 10.1021/acschembio.1c00256

Uniprot ID: Q9H0E9

Target Class: Epigenetic

Target SubClass: Bromodomain

Potency: Kd

Potency Value: 34 nM

Potency Assay: BromoKdELECT (DiscoveRx).

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

Target aliases:

Bromodomain-containing protein 8, SMAP2, SMAP, BRD ...

DOI Reference: 10.1021/acschembio.1c00256

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): Chemoproteomics data showed only BRD8 associated proteins. Selective BD1 over BD2 (Kd >1 uM) in BromoKdELECT (DiscoveRx). High selectivity over BRD9 and BRD4 (IC50s >10 uM ) in biochemical AlphaScreen assays and in-cell engagement within BRET displacement assays. DiscoveRx BromoMax competition panel with DN02 showed minimal off-target engagement across the bromodomain family.

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SERP+ Ratings

In Cell Rating

(last updated: 23 Sept 2024 )