CY-09, exhibits a dose-dependent inhibitory effect on monosodium urate (MSU), nigericin, ATP-induced caspase-1 activation and IL-1β secretion at the doses of 1 to10 μM in LPS-primed bone marrow-derived macrophages (BMDMs). CY-09 is an NLRP3 inhibitor.
CY-09 is an NLRP3 inflammasone inhibitor. CY-09 binds directly to the ATP-binding motif of NLRP3 NACHT domain and inhibits its ATPase activity, blocking NLRP3 inflammasome assembly and activation. In mouse models CY-09 showed therapeutic effects in type 2 diabetes and cryopyrin-associated auto-inflammatory syndrome (CAPS), which is caused by gain-of-function mutations of NLRP3.
