CY-09

CY-09 is a NOD-like receptor protein 3 (NLRP3) inhibitor.¹ It selectively inhibits NLRP3 ATPase activity over the ATPase activity of NLRP1, NLRC4, NOD2, and RIG-I at 1 µM. CY-09 binds directly to the ATP-binding motif of the NLRP3 NACHT domain (K_d = 500 nM) and suppresses NLRP3 inflammasome assembly. It inhibits NLRP3 inflammasome activation induced by nigericin (Item No. 11437) in THP-1 cells when used at a concentration of 1 µM. CY-09 (5 mg/kg, i.p.) improves the left ventricle ejection fraction (LVEF) and left ventricle fractional shortening (LVFS) and reduces myocardial fibrosis in a mouse model of myocardial infarction induced by left anterior descending (LAD) coronary artery occlusion.² It also reduces hepatic steatosis in a high-fat diet-induced mouse model of non-alcoholic fatty liver disease (NAFLD) when administered at a dose of 2.5 mg/kg.³

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1. Jiang, H., He, H., Chen, Y., et al. Identification of a selective and direct NLRP3 inhibitor to treat inflammatory disorders. J. Exp. Med. 214(11), 3219-3238 (2017).

2. Gao, R.-F., Li, X., Xiang, H.-Y., et al. The covalent NLRP3-inflammasome inhibitor Oridonin relieves myocardial infarction induced myocardial fibrosis and cardiac remodeling in mice. Int. Immunopharmacol. 90, 107133 (2021).

3. Wang, X., Sun, K., Zhou, Y., et al. NLRP3 inflammasome inhibitor CY-09 reduces hepatic steatosis in experimental NAFLD mice. Biochem. Biophys. Res. Commun. 534, 734-739 (2021).