CPTH6 is a thiazole derivative that inhibits the lysine acetyltransferase activity of Gcn5 and pCAF but not p300 or CBP.
1 It blocks the acetylation of H3/H4 histones and α-tubulin in several leukemia cell lines.
1 CPTH6 reduces cell viability, arresting cell cycling in the G
0/G
1 phase and inducing apoptosis.
1 It impairs autophagy in a variety of tumor cell lines, at least in part by altering ATG7-mediated elongation of autophagosomal membranes.
2
1. Trisciuoglio, D., Ragazzoni, Y., Pelosi, A., et al. CPTH6, a thiazole derivative, induces histone hypoacetylation and apoptosis in human leukemia cells Clin. Cancer Res. 18(2),475-486(2012).
2. Ragazzoni, Y., Desideri, M., Gabellini, C., et al. The thiazole derivative CPTH6 impairs autophagy Cell Death Dis. 4(3),e524(2013).