hCAIX/XII-IN-1, a potent inhibitor of both CAIX and CAXII, exhibits KI values of 0.48 μM for CAIX and 0.83 μM for CAXII, respectively. This compound demonstrates antiproliferative activity in vitro and induces apoptosis in MCF-7 cells [1].

hCAIX/XII-IN-1, also referred to as compound 11a, demonstrates antiproliferative effects at various concentrations (3.125, 6.25, 12.5, 25, 50 μM over 48 hours) with an IC50 value of 0.48 μM in MCF-7 cells. Additionally, at a concentration of 0.48 μM over 24 hours, it significantly increases the sub-G1 phase cell populations, indicating a disruption in cell cycle progression. Furthermore, at the same concentration, hCAIX/XII-IN-1 induces apoptosis in MCF-7 cells, confirming its efficacy in promoting cell death. These observations were confirmed through cell proliferation assay, cell cycle analysis, and apoptosis analysis, underscoring the compound's potential as a therapeutic agent [1].