top-1 inhibitor 1

Top1 inhibitor 1 is a potent inhibitor of human topoisomerase I (Top1)(IC50: 29 nM).

Top HDAC-IN-1 is a dual topoisomerase (Top) HDAC inhibitor that acts on HDAC1 (IC50: 18 nM), HDAC2 (IC50: 230 nM), HDAC3 (IC50: 790 nM), HDAC6 (IC50: 87 nM) and HDAC8 (IC50: 5250 nM). Top HDAC-IN-1 exhibited potent antitumor effects on HCT116 cells (IC50: 180 nM), blocked the cell cycle of HCT116 cells in G2 phase, and effectively induced apoptosis.

HDAC Top-IN-1 is a broad-spectrum, orally active dual HDAC Top inhibitor that acts on HDAC1 (IC50: 0.036 μM), HDAC2 (IC50: 0.14 μM), HDAC3 (IC50: 0.059 μM), HDAC6 (IC50: 0.089 μM) and HDAC8 ( IC50: 9.8 μM). HDAC Top-IN-1 was able to block HEL cells in S-phase and effectively induce apoptosis.