Drug intelligence / Profile preview

TC-E101

Development stage
Unknown
Lead developer
Tocris
Modality
Small Molecules
Administration
Oral
01

Overview

TC-E101 is a potent and selective small molecule inhibitor of the histone acetyltransferases **p300** (EP300) and **CREB-binding protein** (CBP). It functions by competitively binding to the acetyltransferase domain of these transcriptional co-activators, thereby preventing the acetylation of histone tails and non-histone proteins such as p53 and GATA1. This epigenetic modulation leads to the suppression of oncogenic gene expression programs, particularly those driven by androgen receptors or other transcription factors. TC-E101 is primarily utilized as a pharmacological tool in preclinical oncology research to investigate the therapeutic potential of p300/CBP inhibition in various malignancies, including prostate cancer and hematological cancers.

02

Targets

EP300 (Histone acetyltransferase p300)CREBBP (CREB-binding protein)

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