MS436

Inhibitor of BRD4, BRD3

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe MS436 is in the process of SERP review.

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Information

BRD4
BRD3

Inhibitor

up to 10 uM

Probe Availability:

In Vitro Validations

Uniprot ID: O60885

Target Class: Epigenetic

Target SubClass: Bromodomain

Potency: Ki

Potency Value: 85 nM BD1; 340 nM BD2

Potency Assay: in vitro fluorescent anisotropy binding assay

PDB ID for probe-target interaction (3D structure): 4NUD

Structure-activity relationship: yes

Target aliases:

Bromodomain-containing protein 4, HUNK1, BRD4, BRD ...

DOI Reference: 10.1021/jm401334s

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): in vitro fluorescent anisotropy binding assay

Probe Selectivity in Vitro:

Selectivity against a panel of Bromodomains (Ki - uM): BRD4-BD2 0.34, BRD3-BD1 0.10, BRD3-BD2 0.14, related targets, BRD2 and BRDT were not tested, but are likely to bind MS436; CBP BrD 2.18, PCAF 5.52, BRD7 2.72, BPTF 6.06, BAZ2b 3.29, SMARCA4 7.97

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SERP ratings and comments

SERP+ Ratings

In Cell Rating

SERP+ Comments:

This is an early probe with limited selectivity over the BD2 domain. Probes with better selectivity and cellular activity are available (GSK789, GSK778). No negative control is available. Little cytotoxicity was oberved in MTT assay in murine macrophage RAW264.7 cells.

(last updated: 23 Sept 2024 )