Drug intelligence / Profile preview

A-485

Development stage
Preclinical
Lead developer
Structural Genomics Consortium
Modality
Small Molecules
Administration
Oral, Intraperitoneal (preclinical Research)
01

Overview

**A-485** is a potent and selective small molecule inhibitor of the **p300/CBP histone acetyltransferase (HAT) domain**. It directly inhibits the enzymatic activity of the transcriptional co-activators p300 and CBP, leading to suppression of acetylation of histone H3 at lysine 18 and 27 (H3K18ac, H3K27ac)[4][7][8]. This drug exhibits **anti-proliferative, pro-apoptotic, and epigenetic modulating effects** in cancer models by blocking the transcriptional activation of key oncogenic programs, notably in castration-resistant prostate cancer and several hematologic malignancies[2][4][3]. It reduces inflammatory gene expression, impairs macrophage infiltration, and has demonstrated efficacy in preclinical models of acute liver injury and growth hormone-secreting pituitary adenomas[1][3]. A-485 is orally bioavailable and shows high selectivity for p300/CBP HAT over other acetyltransferases[4][7]. Development has primarily focused on cancer and acute inflammatory diseases.

Brand names
A-485A485A 485
Other names
A 485A485A-485CAS 1889279-16-6CAS1889279-16-6CAS-1889279-16-6
02

Targets

EP300 (Histone acetyltransferase p300)

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