A glucosylceramide synthase inhibitor (IC50 = 40 nM for inhibition of glucosylceramide production in K562 cells); selective for glucosylceramide synthase over α-glucosidase I and II

Eliglustat (hemitartrate) – 1 mg

Brand:
Cayman
CAS:
928659-70-5
Storage:
-20
UN-No:
Non-Hazardous - /

Eliglustat is an inhibitor of glucosylceramide synthase (IC50 = 40 nM for inhibition of glucosylceramide production in K562 cells).{41053} It is selective for glucosylceramide synthase over α-glucosidase I and II, α-1,6-glucosidase, lysosomal glucocerebrosidase, non-lysosomal glucosylceramidase, sucrase, and maltase (IC50s = >10 µM for all). It decreases cell surface levels of the gangliosides GM1 and GM3 in K562 and B16/F10 cells with IC50 values of 24 and 29 nM, respectively. Eliglustat (150 mg/kg per day) decreases glucosylceramide levels in the liver and lungs of D409V/null mice, a model of Gaucher disease. Formulations containing eliglustat have been used in the treatment of type 1 Gaucher disease.  

 

Out of stock

Add to quotes
SKU: 21487 - Category:

Description

A glucosylceramide synthase inhibitor (IC50 = 40 nM for inhibition of glucosylceramide production in K562 cells); selective for glucosylceramide synthase over α-glucosidase I and II, α-1,6-glucosidase, lysosomal glucocerebrosidase, non-lysosomal glucosylceramidase, sucrase, and maltase (IC50s = >10 µM for all); decreases GM1 and GM3 cell surface levels in K562 and B16/F10 cells (IC50s = 24 and 29 nM, respectively); decreases glucosylceramide levels in the liver and lungs of D409V/null mice,,

Formal name: N-[(1R,2R)-2-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-hydroxy-1-(1-pyrrolidinylmethyl)ethyl]-octanamide, 2R,3R-dihydroxybutanedioate (2:1)

Synonyms:  Genz-112638

Molecular weight: 479.6

CAS: 928659-70-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Sphingolipid Turnover||Research Area|Endocrinology & Metabolism|Inborn Errors of Metabolism||Research Area|Lipid Biochemistry|Sphingolipids||Research Area|Neuroscience

Related products

  • CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}

    CAY10512 – 50 mg

    The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}  

     

    Brand:
    Cayman
    SKU:10009536 - 50 mg

    Available on backorder

    Add to quotes
    View product page
  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 50 mg

    The tetracycline repressor (TetR) is a transcriptional regulator which normally binds tightly to its palindromic tetO operator DNA, blocking gene expression.{17508} Tet causes the repressor to dissociate from the DNA, allowing transcription to occur. A novel reverse TetR (revTetR) requires tetracycline as a co-repressor to bind tetO and block transcription.{17509,17510} Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet.{17508,17511} Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet,{17512} so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.{17508}  

     

    Brand:
    Cayman
    SKU:10009542 - 50 mg

    Available on backorder

    Add to quotes
    View product page
  • CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}

    CAY10512 – 500 mg

    The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}  

     

    Brand:
    Cayman
    SKU:10009536 - 500 mg

    Available on backorder

    Add to quotes
    View product page
  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 10 µg

    The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.  

     

    Brand:
    Cayman
    SKU:10009531 - 10 µg

    Available on backorder

    Add to quotes
    View product page