Drug intelligence / Profile preview

BRD4770

Development stage
Discontinued
Lead developer
Broad Institute
Modality
Small Molecules
Administration
Intraperitoneal, Oral, Infusion, Bolus Injection
01

Overview

BRD4770 is a small molecule inhibitor of the histone methyltransferase G9a (also known as EHMT2). It was structurally derived from BIX-01338 and acts by reducing the di- and trimethylation of lysine 9 on histone H3 (H3K9). Primarily used as a research tool, BRD4770 has demonstrated preclinical activity in inducing senescence in pancreatic cancer cells and protecting against doxorubicin-induced cardiotoxicity by inhibiting cardiomyocyte ferroptosis and apoptosis. It has also been investigated for its potential to enhance NK cell-mediated anti-tumor immunity through the suppression of TGF-β1. The compound is not currently approved for human use and is not being developed by a specific pharmaceutical company for a therapeutic indication.

02

Targets

EHMT2SETD8 (Lysine methyltransferase 5A)SUV39H2 (Histone-lysine N-methyltransferase SUV39H2)

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