Z-WEHD-FMK is a cell-permeable and irreversible inhibitor of caspase-1/5. It also shows a robust inhibitory effect on cathepsin B activity (IC50: 6 μM).

Z-WEHD-FMK (80 μM; 9 hours) nearly completely blocks C. trachomatis-induced cleavage of golgin-84 and increases GM130 expression in cells [1]. Administered 30 minutes before exposure to E. piscicida, Z-WEHD-FMK effectively inhibits 0909I E. piscicida-induced ZF4 cell cytotoxicity and pyroptotic morphology [2]. Z-WEHD-FMK (20 μM; 18-24 hours following exposure to Cr3+, Ni2+, and Co2+) significantly reduces IL-1β release in bone marrow-derived macrophages by 76% to 86% with 200 to 400 ppm Cr3+, by 35% to 45% with 48 ppm or higher Ni2+, and below detection threshold with 6 ppm Co2+, as well as by 40% to 48% with 12 to 24 ppm Co2+ [3].