MMP2-IN-1 shows siganificant antiproliferative activity in certain cancer cells through arresting the cell cycle and inducing apoptosis. MMP2-IN-1 is a moderate potenet inhibitor of MMP2 (IC 50 = 6.8 μM)[1].

MMP2-IN-1 (compound 4a) demonstrated potent anticancer activity in various cancer cell lines. At concentrations ranging from 0-10 μM over 74 hours, it exhibited half-maximal inhibitory concentrations (IC50) of 0.07 μM, 0.11 μM, and 0.18 μM against MDA-MB-231, A549, and HeLa cancer cells, respectively, while showing minimal effectiveness in Hep 5G cells at over 10 μM. Additionally, a concentration of 10 μM induced S phase cell cycle arrest in MDA-MB-231 cells after 24 hours. MMP2-IN-1 also promoted a dose-dependent increase in both early and late-stage apoptosis in MDA-MB-231 cells, enhancing early-stage apoptosis from 4.66% to 10.9% at a concentration of 10 μM after 24 hours.

MMP2-IN-1, when administered intraperitoneally (IP) in single doses of 100 mg/kg, 150 mg/kg, 200 mg/kg, and 250 mg/kg to Kunming mice (n=10, evenly split between male and female), exhibited increasing mortality rates of 0%, 30%, 50%, and 60% respectively [1]. Conversely, a daily IP administration of 10 mg/kg MMP2-IN-1 over 14 days significantly inhibited tumor growth in an orthotopic 4T1 tumor-bearing mouse model, showcasing its potential in treating metastatic 4T1 murine breast cancer [1].