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GSK-2801

Development stage: Preclinical
Lead developer: GSK
Modality: Small Molecules
Administration: Oral

Overview

GSK-2801 is a potent, selective, and orally active small molecule chemical probe developed by GSK. It functions as an acetyl-lysine competitive inhibitor of the BAZ2A and BAZ2B bromodomains, which are critical scaffolding proteins within the nucleolar remodeling complex (NoRC) that regulates noncoding RNA expression. GSK-2801 is primarily utilized as a research tool to investigate the role of BAZ2 bromodomains in chromatin biology and epigenetic regulation. Preclinical research has demonstrated its potential in sensitizing triple-negative breast cancer cells to BET inhibitors and reversing paclitaxel resistance in anaplastic thyroid cancer via MYCN downregulation. It is not intended for human therapeutic use.

Other names: CAS 1619994-68-1CAS1619994-68-1CAS-1619994-68-1

Targets

BRD9 (Bromodomain-containing protein 9)BAZ2A (Bromodomain adjacent to zinc finger domain protein 2A)BAZ2B (Bromodomain adjacent to zinc finger domain protein 2B)

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