hCAIX-IN-12 is an effective hCAIX inhibitor, IC50 for CAIX and CAII is 0.74 and 10.78 μM , respectively. hCAIX-IN-12 inhibits cell proliferation and induces apoptosis. HCAIX-IN-12 can increase the generation of ROS. HCAIX-IN-12 has research potential in colorectal cancer (CRC).

hCAIX-IN-12 (compound OX27) demonstrates antiproliferative effects on HCT-116 cells with an IC50 value of 6.0 μM [1], significantly reducing CAIX expression under hypoxic conditions [1]. It inhibits HCT-116 cell colony formation and migration in a dose- and time-dependent manner [1], triggers apoptosis, and increases reactive oxygen species (ROS) levels at 6.0 μM after 24 and 48 hours [1]. Additionally, hCAIX-IN-12 disrupts the cell cycle, decreasing the G0/G1 phase population (65.21%) and accumulating cells in the G2/M phase (18.95%) [1]. It exhibits high binding affinity to CAIX and significant affinity to human serum albumin (HSA) [1].