CPTH6, a thiazole derivative, selectively inhibits the lysine acetyltransferase activity of Gcn5 and pCAF without affecting p300 or CBP. It effectively blocks the acetylation of H3/H4 histones and α-tubulin in various leukemia cell lines, leading to reduced cell viability by arresting the cell cycle in the G0/G1 phase and inducing apoptosis. Additionally, CPTH6 disrupts autophagy across several tumor cell lines, primarily by interfering with ATG7-mediated autophagosomal membrane elongation.