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-17020S
    Miglustat-d9
    Miglustat-d9 is the deuterium labeled Miglustat. Miglustat (N-Butyldeoxynojirimycin) is an inhibitor of glucosylceramide synthase, primarily to treat Type I Gaucher disease (GD1).
    Miglustat-d<sub>9</sub>
  • HY-116535C
    D-threo-PPMP
    D-threo-PPMP is a potent inhibitor of glucosylceramide (GlcCer) synthase. D-threo-PPMP can block karyokinesis and reduce cyst production.
    D-threo-PPMP
  • HY-144270
    Glucosylceramide synthase-IN-3
    Glucosylceramide synthase-IN-3 (compound BZ1) is a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC50s of 16 nM for human GCS.Glucosylceramide synthase-IN-3 can be used for Gaucher's disease research.
    Glucosylceramide synthase-IN-3
  • 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-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-12744A
    Genz-123346
    Genz-123346 is a potent, orally available glucosylceramide synthase inhibitor. Genz-123346 blocks the conversion of ceramide to glucosylceramide (GL1) and inhibits GM1 with an IC50 value of 14 nM.
    Genz-123346
Cat. No. Product Name / Synonyms Application Reactivity