IDE Inhibitor

6bK TFA is a selective insulin-degrading enzyme (IDE) inhibitor with an IC₅₀ of 50 nM. 6bK TFA binds to the distal pocket of IDE, thereby blocking substrate binding, peptide unfolding and cleavage processes, and reducing the degradation of insulin, glucagon and amylin. 6bK TFA improves oral glucose tolerance but impairs intraperitoneal glucose tolerance. 6bK TFA can be used in research related to type 2 diabetes.

ML345 is a potent and selective inhibitor of insulin-degrading enzyme (IDE) and NLRP3, with an IC₅₀ of 188 nM against IDE. ML345 targets the Cys819 residue of IDE to inhibit IDE. ML345 selectively binds to NLRP3 in a non-covalent manner. ML345 inhibits inflammatory cytokines (IL-1β, IL-6) and exhibits potent anti-inflammatory activity. ML345 exerts a protective effect against miscarriage.

IDE-IN-2 (Compound 4) is an inhibitor for insulin-degrading enzyme. IDE-IN-2 is predicted to have CYP3A4, CYP2C19, hERG, NADP+, HIF1α and histidine kinase inhibitory activities, and has potential biological activity in anti-diabetic, anti-tumor, anti-bacterial aspects, according to the in silico prediction.

6bK formate is a potent and selective insulin degrading enzyme (IDE) inhibitor with an IC₅₀ value of 50 nM. 6bK formate increases circulating insulin in high-fat-fed mice. Acute administration of 6bK formate enhances glucose tolerance to oral glucose, notably to a greater extent in high-fat-fed mice. 6bK formate can be used for type 2 diabetes research.