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 (0-500 μM; 1 hour; MCF7 cells) treatment significantly reduces the viability of MCF7 cells[1]. TH1834 (0-500 μM; 1 hour; MCF7 cells) treatment significantly increases cytotoxicity in MCF7 cells[1]. TH1834 (500 μM; 1 hour; MCF7 cells) treatment induces caspase 3 activation in MCF7 cells[1]. TH1834 significantly inhibits Tip60 activity in vitro and treating cells with TH1834 results in apoptosis and increased unrepaired DNA damage in breast cancer[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.