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BAY 299
- Development stage
- Preclinical
- Lead developer
- Bayer
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
BAY 299 is a potent and selective small molecule inhibitor of the bromodomains of BRPF2 (also known as BRD1) and TAF1. Developed as part of a collaboration between Bayer and the Structural Genomics Consortium (SGC), it serves as a chemical probe to study epigenetic signaling. In preclinical studies, BAY 299 has demonstrated significant anti-proliferative activity in marginal zone lymphoma (MZL) models, including those with acquired resistance to targeted therapies like BTK, BCL2, and PI3K inhibitors. Its mechanism involves disrupting the interaction of BRPF2 and TAF1 with acetylated histones, thereby modulating transcriptional networks involved in lymphomagenesis.
02
Targets
TAF1L-BD2 (Transcription initiation factor TFIID subunit 1-like bromodomain 2)BRPF2 (Bromodomain and PHD finger-containing protein 2)Transcription initiation factor TFIID subunit 1 bromodomain 2
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