TH1834 dihydrochloride

TH1834 dihydrochloride (TH-1834, TH 1834) is a novel potent specific histone acetyltransferase Tip60 inhibitor; induces apoptosis in breast cancer cell lines with more cytotoxicity than staurosporine; increases the γH2AX foci in the cancer cell lines PC-3 and DU-145 combined with IR; induces apoptosis and increases unrepaired DNA damage in breast cancer cells.

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Histone Acetyltransferase

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 highly significant increase in cytotoxicity[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.

[1]. Gao C, et al. Rational design and validation of a Tip60 histone acetyltransferase inhibitor. Sci Rep. 2014 Jun 20;4:5372.