A1874

A1874 : Degrader (PROTAC) of BRD4

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe A1874 is in the process of SERP review.

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Information

BRD4

Degrader (PROTAC)

100 nM
Reviewer recommended concentration: 100 nM to 1 µM

Probe Availability:

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

No in Vivo Validations

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

This is a potent degrader of BRD4. Although many BRD4 PROTACS exist, this is one of the first to use MDM2 as the E3 ligase. MDM2-mediated degradation has been demonstrated via control experiments. However, to further improve the usefulness of this probe, proteomics experiments to show the selectivity would be useful as well as an assessment of the degradation time course. The compound is therefore a useful orthogonal chemical probe.

(last updated: 20 Feb 2025 )