GlcCer Synthase Inhibitor Development Service

GlcCer Synthase Inhibitor Development Service

Glucosylceramide Synthase (GCS) Inhibitor Development Service at CD BioGlyco

CD BioGlyco is experienced in the development of Glycosphingolipid Inhibitors. GCS glycosylates ceramide to glucose ceramide, thereby reducing the pro-apoptotic effects of ceramide. GCS is overexpressed in a variety of drug-resistant cancer cells. The use of GCS inhibitors as a way to block ceramide glycosylation is expected to provide new ideas for cancer therapy research. Several GCS Inhibitors have been developed. Based on published reports and our extensive experience in Glycosylation Inhibitor Development, we offer multi-faceted GCS Inhibitor development services.

Fig.1 Directions for GCS inhibitor development. (CD BioGlyco)Fig.1 Directions for GCS inhibitor development. (CD BioGlyco)

  • Natural product-based GCS inhibitor development services
    There may be some natural products in plants and bacteria that have inhibitory effects on GCS. We screen compounds with better inhibitory effects from many natural products. To improve the efficiency of GCS inhibitors, we construct a high-throughput screening system. We will perform a series of tests on the screened compounds, including their inhibitory effects on GCS, mechanisms of action, etc. We aim to screen GCS inhibitors with better effects.
  • Substrate analog-based GCS inhibitor development services
    Substrate Analogs will compete with the substrate to bind to the key site of GCS, thus achieving the purpose of inhibiting its activity. Several inhibitors based on GCS substrate analogs, such as eliglustat, miglustat, etc., have been developed. We will simulate the chemical structure of GCS substrate and screen compounds with strong inhibitory activity against GCS based on this structure.
  • Inhibitor development services in other directions
    We modify the structures of published GCS inhibitors, such as (R, R)-(D-threo)-isomer of 1-phenyl-2-decanoylamino-3-morpholino-1-propanol, etc. We aim to synthesize compounds with greater selectivity and inhibitory effect.


Technology: High-throughput screening systems

Journal: Journal of Neurochemistry


Published: 2021

Results: In this study, a high-throughput screening system was constructed for the study of GCS inhibitors. A novel potent inhibitor, T-036, was successfully identified. It has a different chemical structure from the reported GCS substrate mimetic inhibitors and does not contain aliphatic amine moiety. It was detected to achieve inhibition by non-competitive binding to UDP-glucose. The inhibitory ability of T-036 was further verified by mouse experiments.

Fig.2 Chemical structure of T-036. (Fujii, et al., 2021)Fig.2 Chemical structure of T-036. (Fujii, et al., 2021)


  • The activity of GCS affects the function of sphingolipids in cells. The development of GCS inhibitors is used to study the function and metabolism of sphingolipids in cells.
  • GCS plays a role in the development of multidrug resistance (MDR) in cancer cells. The development of GCS inhibitors has a crucial role in the study of the MDR reversal mechanism.
  • The development of GCS inhibitors provides new ideas for the study of lipid storage disorder therapy.


  • We have constructed a specialized high-throughput screening system, which greatly improves the efficiency of GCS inhibitor development.
  • Our inhibitor development services for GCS cover multiple directions, including screening and research on substrate analogs and natural products, etc.
  • Our researchers are experienced in chemical synthesis. Modification of existing GCS inhibitors is easily realized.

At CD BioGlyco, our glycosylation inhibitor development process keeps up with scientific developments and is constantly updated. We have an experienced research team in inhibitor development to provide high-quality and reliable inhibitor development services. Please feel free to contact us to learn more about GCS inhibitor development. Our researchers will get back to you as soon as possible.


  1. Fujii, T.; et al. A new brain-penetrant glucosylceramide synthase inhibitor as potential Therapeutics for Gaucher disease. J Neurochem. 2021, 159(3): 543-553.
This service is for Research Use Only, not intended for any clinical use.

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