In Vitro: NLRP3/AIM2-IN-3 (0-100 μM) displays remarkable inhibitory activity against NLRP3-and AIM2-but not NLRC4-dependent activation of caspase-1 and the release of IL-1b in human THP-1 macrophages. NLRP3/AIM2-IN-3 shows inhibition of IL-1b secretion by human THP-1 macrophages, with IC50 of 0.098 μM, which is nearly 150-fold and 500-fold more potent than that of J774A.1 (14.62 μM) and bone marrow-derived macrophages (BMDMs) (48.98 μM), respectively. NLRP3/AIM2-IN-3 has almost no inhibitory effect on the AIM2 inflammasome-dependent activation of caspase-1 and release of IL-1b in J774A.1 cells.