hCAIX-IN-12

hCAIX-IN-12 is a potent hCAIX inhibitor with IC50 values of 0.74, 10.78 µM for CAIX and CAII, respectively. hCAIX-IN-12 shows antiproliferative effect and induces apoptosis. hCAIX-IN-12 increases ROS production. hCAIX-IN-12 has the potential for the research of colorectal cancer (CRC) [1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> Carbonic Anhydrase

IC50: 0.74 µM (CAIX); 10.78 µM (CAII)[1].

hCAIX-IN-12 (compound OX27) shows antiproliferative effect with IC50s of 6.0 µM for HCT-116 cells[1]. hCAIX-IN-12 decreases the expression of CAIX in HCT-116 cells and inhibits the expression of CAIX more pronouncedly in hypoxic conditions[1]. hCAIX-IN-12 (0-50 µM; 0-48 h) inhibits the colony formation in a dose-dependent manner and 7 inhibits the migration of HCT-116 cells[1]. hCAIX-IN-12 (6.0 µM; 48 h) induces apoptosis in HCT-116 cells[1]. hCAIX-IN-12 (6.0 µM; 24,48 h) increases in the levels of ROS in HCT-116 cells[1]. hCAIX-IN-12 causes depletion of HCT-116 cells in the G0/G1 (P2 65.21%) phase with an increase in the accumulation of cells in G2/M (P4 18.95%) phase[1]. hCAIX-IN-12 has high binding affinity for CAIX and substantial affinity for HSA[1].

[1]. Shamsi F, et al. Synthesis and SAR studies of novel 1,2,4-oxadiazole-sulfonamide based compounds as potential anticancer agents for colorectal cancer therapy. Bioorg Chem. 2020 May;98:103754.