CHI-KAT8i5 is a selective, orally active inhibitor of KAT8 (lysine acetyltransferase 8) designed for oncology research. It shows measurable binding to KAT8, inhibits proliferation of esophageal cancer cell lines in vitro, induces dose-dependent apoptosis, and has demonstrated tumor growth suppression in xenograft models.
- Selective KAT8 inhibition with a measured KD of 19.72 μM.
- Cellular antiproliferative activity (IC50 2-3 μM) in esophageal cancer cell lines.
- Induces dose-dependent apoptosis in treated cells.
- Reduces H4K16ac and c-Myc levels in cellular assays.
- Demonstrated oral activity and tumor growth suppression in vivo.
- High DMSO solubility (100 mg/mL) and defined storage recommendations.