MCC950 sodium

MCC950 sodium salt is a potent, selective inhibitor of NOD-like receptor family protein 3 (NLRP3) with IC50 value of 7.5 nM in bone marrow derived macrophages (BMDMs) [1].

MCC950 effectively and selectively inhibits NLRP3 which is involved in various biological processes including autoinflammatory and autoimmune diseases. MCC950 is thus a potential therapeutic for NLRP3-associated syndromes, and a tool for the further study of the NLRP3 inflammasome in human health and disease [1].

In BMDM and human monocyte derived macrophage (HMDM) cells, MCC950 specifically inhibited canonical and noncanonical NLRP3 activation at IC50 of 7.5 nM and 8.1 nM, respectively, without affecting absent in melanoma 2 (AIM2), NOD-like receptor family CARD domain containing protein 4 (NLRC4) or NLRP1 inflammasomes [1].

In mice intraperitoneally injected with lipopolysaccharides (LPS), pre-treatment with MCC950 (50 mg/kg, i.p., 1 h before LPS injection) reduced serum concentrations of interleukin-1β (IL-1β) and IL-6 while it did not considerably decrease the amount of tumor necrosis factor-α (TNF-α). MCC950 attenuated the severity of experimental autoimmune encephalomyelitis [1].

Reference:

[1]. Coll R C, Robertson A A, Chae J J. A small-molecule inhibitor of the NLRP3 inflammasome for the treatment of inflammatory diseases. Nature Medicine, 2015, 21(3): 248-255.