INF39

INF39 is an irreversible inhibitor of the NLRP3 inflammasome.¹ INF39 (10 µM) inhibits activation of caspase-1 and the release of IL-1β and lactate dehydrogenase (LDH) induced by ATP (Item No. 14498) or nigericin (Item No. 11437) in LPS-primed bone marrow-derived macrophages (BMDMs). It reduces ATP-induced pyroptosis in LPS-primed THP-1 cells by 33.6% when used at a concentration of 10 µM. INF39 (12.5, 25, and 50 mg/kg) prevents increases in IL-1β protein levels induced by dinitrobenzene sulfonic acid (DNBS) in the colon in a rat model of colitis. It reduces the severity of pancreatic lesions and serum levels of IL-1β, TNF-α, and IL-6 during caerulein- and LPS-induced pancreatitis in mice when administered at doses of 25 and 50 mg/kg.²

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1. Cocco, M., Pellegrini, C., Martínez-Banaclocha, H., et al. Development of an acrylate derivative targeting the NLRP3 inflammasome for the treatment of inflammatory bowel disease. J. Med. Chem. 60(9), 3656-3671 (2017).

2. Fu, Q., Zhai, Z., Wang, Y., et al. NLRP3 deficiency alleviates severe acute pancreatitis and pancreatitis-associated lung injury in a mouse model. Biomed. Res. Int. 1294951, (2018).