NLRP3/AIM2-IN-3 (compound 59) is a potent inhibitor with differential species specific effects against NLRP3 and AIM2 inflammasome-dependent pyroptosis . NLRP3/AIM2-IN-3 shows inhibitory efficacy against pyroptosis in THP-1 macrophages stimulated with LPS/nigericin, with an IC 50 of 0.077 ± 0.008 μM. NLRP3/AIM2-IN-3 disturbs the interaction of NLRP3 or AIM2 with the adaptor protein ASC and inhibited ASC oligomerization
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 IC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.