Search by product name, CAS, target or catalog number. Press Down Arrow to reach product suggestions, Tab to move between links, and Escape to close suggestions.
Glucosylceramide synthase (GCS) inhibitors block the first step in glycosphingolipid synthesis. The enzyme, encoded by the ceramide glucosyltransferase gene (UGCG), transfers glucose to ceramide on the cytosolic face of the Golgi. Glucosylceramide is the precursor of lactosylceramide and of most complex glycosphingolipids, including gangliosides. Blocking its formation lowers glycolipid storage in models of Gaucher disease and other lysosomal storage disorders, an approach known as substrate reduction. Because GCS also consumes ceramide, inhibitors are used to study ceramide signaling and drug resistance in cancer cells. Listed compounds include the ceramide analogs D-threo-PDMP, Genz-123346 and eliglustat, the iminosugar miglustat hydrochloride, and ibiglustat.
EXEL-0346 is a potent glucosylceramide synthase (GCS) inhibitor, demonstrating an IC50 value of 2 nM. This compound enhances insulin signaling through an increase in pAkt levels while effectively decreasing the concentrations of glucosylceramide, lactosylceramide, and GM3. EXEL-0346 shows promise in addressing metabolic disorders, particularly obesity and diabetes, making it a valuable tool for research in these areas.
Out of stock
All 3 sizes
Glucosylceramide synthase-IN-4 is a potent inhibitor of glucosylceramide synthase (GCS), exhibiting an IC50 value of 6.8 nM. This compound demonstrates favorable pharmacokinetic properties and stability in human hepatocytes, making it suitable for in vitro studies. Additionally, Glucosylceramide synthase-IN-4 exhibits effective central nervous system (CNS) penetration and maintains acceptable selectivity for PXR, facilitating research into GCS-related pathways and potential therapeutic applications in metabolic disorders.
Out of stock
All 3 sizes
FUT8-IN-1 is a potent inhibitor of α-1,6-fucosyltransferase (FUT8), exhibiting a KD of 49 nM and an IC50 of approximately 50 µM. This compound generates a highly reactive naphthoquinone imine intermediate upon interaction with FUT8, effectively inhibiting its enzymatic activity. FUT8-IN-1 is valuable for investigating the role of FUT8 in glycosylation processes and its implications in various biological research applications.
Out of stock
All 3 sizes