Chst15-IN-1 is a selective, reversible, covalent inhibitor of the Chst15 enzyme that suppresses sulfation of chondroitin sulfate-E (CS-E) and related sulfotransferases, attenuating the inhibitory effects of chondroitin sulfate proteoglycans (CSPGs) and making it a promising candidate for promoting neuronal repair.

Chst15-IN-1, when acting on Neu7 astrocytes at a concentration of 25 μM for 24 hours, exhibits selectivity towards sulfotransferase, which is significantly higher than its selectivity towards various proteins containing active cysteine residues. At concentrations of 10 μM and 25 μM, Chst15-IN-1 significantly reduces the expression level of chondroitin sulfate-E (CS-E) on the cell surface of Neu7 astrocytes, with this reduction effect demonstrating a dose-dependent manner [1].

Chst15-IN-1, when administered intravenously (i.v.) at a dose of 3.0 mg/kg, exhibits the following pharmacokinetic characteristics: moderate clearance with a value of 21 mL/(min・kg); moderate volume of distribution with a value of 0.97 L/kg; and a relatively short terminal half-life with a value of 1.6 hours [1].