HDAC-IN-92 is a pan-HDAC inhibitor with an IC50 of 12.58 µM in A2780 cells. It exhibits broad and significant cytotoxic activity against various human cancer cell lines, including ovarian, liver, and breast cancer. HDAC-IN-92 induces apoptosis and significantly inhibits tumor cell colony formation. It can also suppress the formation of blood vessels in the chicken chorioallantoic membrane (CAM). In 4T1 tumor-bearing mouse models, HDAC-IN-92 demonstrates antitumor effects and is suitable for research targeting solid tumors.

HDAC-IN-92 (compound 6g) exhibits significant cytotoxicity in various cancer cell lines with IC50 values of 22.17 μM (MCF-7), 8.46 μM (HepG2), 8.10 μM (A2780), 26.89 μM (A2780cis), 75.90 μM (HT29), and 14.11 μM (4T1). The cytotoxicity of HDAC-IN-92 against cancer cells correlates with its pan-HDAC inhibitory activity, suggesting that its antitumor effects are likely mediated by histone deacetylase inhibition. At 8.10 μM for 24 hours, HDAC-IN-92 significantly induces apoptosis in A2780 cells, increasing the total apoptotic cell percentage from 1.82% to 22.17% and effectively inhibiting cell migration. Additionally, at 22.17 μM for 10 days, HDAC-IN-92 notably suppresses colony formation in MCF-7 cancer cells. In the chicken embryo chorioallantoic membrane (CAM) assay, HDAC-IN-92 at 5 μM for 96 hours effectively inhibits angiogenesis, comparable to Vorinostat, as evidenced by reductions in branching points, vessel count, and total vessel length.

HDAC-IN-92 at a dose of 50 mg/kg via intraperitoneal injection every other day for 21 days effectively inhibits tumor growth in a 4T1 tumor BALB/c mouse model, while also demonstrating good tolerability.