TH1834 is a selective inhibitor of the Tip60 (KAT5) histone acetyltransferase (HAT). It effectively induces apoptosis and promotes DNA damage in breast cancer cells. Notably, TH1834 does not influence the activity of the MOF histone acetyltransferase, which is structurally related. Overall, TH1834 exhibits potent anticancer activity.

TH1834 treatment (0-500 μM; 1 hour; MCF7 cells) significantly reduces MCF7 cell viability and increases cytotoxicity. At 500 μM, TH1834 induces caspase 3 activation in MCF7 cells. TH1834 significantly inhibits Tip60 activity in vitro, leading to apoptosis and increased unrepaired DNA damage in breast cancer cells. [1]

Cell Viability Assay[1]
Cell Line: MCF7 cells
Concentration: 0 μM, 0.5 μM, 5 μM, 50 μM, and 500 μM
Incubation Time: 1 hour
Result: Significantly reduced the viability of MCF7 cells.

Cell Cytotoxicity Assay[1]
Cell Line: MCF7 cells
Concentration: 0 μM, 0.5 μM, 5 μM, 50 μM, and 500 μM
Incubation Time: 1 hour
Result: Highly significant increase in cytotoxicity at all concentrations used.

Western Blot Analysis[1]
Cell Line: MCF7 cells
Concentration: 500 μM
Incubation Time: 1 hour
Result: Marked caspase 3 activation was observed in MCF7 cells in an independent assay.