| Description | Chst15-IN-1 is a powerful, reversible, covalent inhibitor of the Chst15 enzyme. It effectively suppresses the sulfation levels of chondroitin sulfate-E (CS-E) and other closely related sulfotransferases responsible for glycosaminoglycans (GAGs) synthesis. Acting as a selective sulfotransferase inhibitor, Chst15-IN-1 can attenuate the inhibitory actions of chondroitin sulfate proteoglycans (CSPGs), making it a promising candidate for enhancing neuronal repair. |
| In vitro | Chst15-IN-1 (25 μM; 24 hours; Neu7 astrocytes) is selective for sulfotransferases over the myriad of reactive cysteine-containing proteins. Chst15-IN-1 (10 and 25 μM; Neu7 astrocytes) shows a significant dose dependent decrease in cell-surface CS-E expression[1]. |
| In vivo | Chst15-IN-1 (3.0 mg/kg; i.v.) has a moderate clearance of 21 mL/min/kg, moderate volume of distribution of 0.97 L/kg, and short terminal half-life of 1.6 hours[1]. Animal Model: Rats Dosage: 3.0 mg/kg (Pharmacokinetic Analysis) Administration: I.v. Result: Had a moderate clearance of 21 mL/min/kg, moderate volume of distribution of 0.97 L/kg, and short terminal half-life of 1.6 h. |
| Synonyms | Chst15-IN-1 |
| molecular weight | 442.09 |
| Molecular formula | C17H11BrCl2N2O3 |
| CAS | 2158198-77-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| References | 1. Cheung ST, et al. Discovery of a Small-Molecule Modulator of Glycosaminoglycan Sulfation. ACS Chem Biol. 2017;12(12):3126-3133. |