2. Signaling Pathways
  3. Neuronal Signaling
  4. Glucosylceramide Synthase (GCS)

Glucosylceramide Synthase (GCS)

Glucosylceramide synthase (GCS), converting ceramide to glucosylceramide, catalyzes the first reaction of ceramide glycosylation in sphingolipid metabolism. This glycosylation by GCS is a critical step regulating the modulation of cellular activities by controlling ceramide and glycosphingolipids (GSLs). An increase of ceramide in response to stresses, such as chemotherapy, drives cells to proliferation arrest and apoptosis or autophagy; however, ceramide glycosylation promptly eliminates ceramide and consequently, these induced processes, thus protecting cancer cells. Furthermore, persistently enhanced ceramide glycosylation can increase GSLs, participating in selecting cancer cells to drug resistance. GCS is overexpressed in diverse drug-resistant cancer cells and in tumors of breast, colon, and leukemia that display poor response to chemotherapy. As ceramide glycosylation by GCS is a rate-limiting step in GSL synthesis, inhibition of GCS sensitizes cancer cells to anticancer drugs and eradicates cancer stem cells.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-116392G
    D,L-erythro-PDMP
    		Inhibitor
    D,L-erythro-PDMP is an erythro isomer of PDMP. D,L-erythro-PDMP causes growth inhibition of cultured rabbit skin fibroblasts. PDMP is an effective inhibitor of UDP-glucose:ceramide glucosyltransferase.
    D,L-erythro-PDMP
  • HY-116392A
    (−)-L-threo-PDMP hydrochloride
    		Inhibitor
    (−)-L-threo-PDMP hydrochloride is the hydrochloride form of (−)-L-threo-PDMP. L-threo-PDMP is a glucosylceramide synthase (GCS) inhibitor. L-threo-PDMP stimulates the proliferation of cultured aortic smooth muscle cells, and that increases the level of LacCer in B16 melanoma cells.
    (−)-L-threo-PDMP hydrochloride
  • HY-112488
    EXEL-0346
    		Inhibitor
    EXEL-0346 is an orally active glucosylceramide synthase (GCS) inhibitor, with an IC50 of 2 nM. EXEL-0346 combined with insulin increases pAkt. EXEL-0346 effectively reduces the levels of Glucosylceramide, Lactosylceramide and GM3. EXEL-0346 improves obesity and diabetes.
    EXEL-0346
  • HY-E70139
    UDP-GalNAc:β-1,3-N-acetylgalactosaminyltransferase 2
    UDP-GalNAc:β-1,3-N-acetylgalactosaminyltransferase 2 ( EC:2.4.1.313; B3GALNT2; β-1,3-N-acetylgalactosaminyltransferase II) is a glycosyltransferase .
    UDP-GalNAc:β-1,3-N-acetylgalactosaminyltransferase 2
  • HY-163131
    Glucosylceramide synthase-IN-4
    		Inhibitor
    Glucosylceramide synthase-IN-4 (compound 12) is a potent glucosylceramide synthase (GCS) inhibitor, with an IC50 of 6.8 nM. Glucosylceramide synthase-IN-4 shows excellent PK properties and stability in human hepatocytes. Glucosylceramide synthase-IN-4 has good CNS penetration and acceptable PXR selectivity.
    Glucosylceramide synthase-IN-4
  • HY-170541
    FUT8-IN-1
    		Inhibitor
    FUT8-IN-1 (Compound 37) is an inhibitor for α-1,6-fucosyltransferase (FUT8) with an KD of 49 nM and an IC50 of ca. 50 µM. FUT8-IN-1 generates a highly active naphthoquinone imine intermediate in the presence of FUT8, and inhibits the enzymatic activity of FUT8.
    FUT8-IN-1
  • HY-17020AR
    Miglustat hydrochloride (Standard)
    		Inhibitor
    Miglustat (hydrochloride) (Standard) is the analytical standard of Miglustat (hydrochloride). This product is intended for research and analytical applications. Miglustat (N-Butyldeoxynojirimycin) hydrochloride is an orally active and reversible ceramide glucosyltransferase inhibitor. Miglustat hydrochloride can be used for the research of type I gaucher disease.
    Miglustat hydrochloride (Standard)
  • HY-17020R
    Miglustat (Standard)
    		Inhibitor
    Miglustat (Standard) is the analytical standard of Miglustat. This product is intended for research and analytical applications. Miglustat (N-Butyldeoxynojirimycin) is an orally active and reversible ceramide glucosyltransferase inhibitor. Miglustat can be used for the research of type I gaucher disease.
    Miglustat (Standard)
  • HY-106392R
    Lucerastat (Standard)
    Lucerastat (Standard) is the analytical standard of Lucerastat. This product is intended for research and analytical applications. Lucerastat, the galactose form of Miglustat, is an orally-available inhibitor of glucosylceramide synthase (GCS). Lucerastat has the potential for Fabry disease study.
    Lucerastat (Standard)
Cat. No. Product Name / Synonyms Application Reactivity