A1874

A1874 : Degrader (PROTAC) of BRD4

Structure

SERP Rating

In Cells

(2 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 )

SERP+ Ratings

In Cell Rating

SERP+ Comments:

This paper identifies a potent MDM2 recruiting PROTAC with nanomolar DC50 and high Dmax reported. Demonstration of identify ternary complex formation would have been desirable. The compound has some potential as an anti-cancer tool with a synergistic MOA , but additional data is necessary. For use as a tool to study BRD4 degradation better BRD4-targeting PROTACs are available.

(last updated: 6 Feb 2026 )