A modulator of γ-secretase that inhibits AICD cleavage to Aβ (IC50s = 531 and 131 nM for Aβ40 and Aβ42

NGP-555 – 5 mg

Brand:
Cayman
CAS:
1304630-27-0
Storage:
-20
UN-No:
Non-Hazardous - /

NGP-555 is a modulator of γ-secretase that inhibits APP intracellular signaling domain (AICD) cleavage to amyloid-β (Aβ; IC50s = 531 and 131 nM for Aβ40 and Aβ42, respectively, in HeLa cell membranes).{48964} It is selective for AICD cleavage to Aβ over E-cadherin and Notch cleavage to their signaling effectors, E-cadherin γ-C-terminal fragment and NICD, respectively, processes also mediated by γ-secretase, when used at a concentration of 30 µM. Dietary administration of NGP-555 (~50 mg/kg per day) reduces cortical and hippocampal plaque area in the Tg2576 transgenic mouse model of Alzheimer’s disease.{48964} NGP-555 (25 mg/kg per day, p.o.) decreases plasma and brain Aβ40 and Aβ42 levels, as well as increases spontaneous alternations in the Y-maze, indicating prevention of memory deficits, in Tg2576 mice.{35879}  

 

Available on backorder

Add to quotes
SKU: 27918 - 5 mg Category:

Description

A modulator of γ-secretase that inhibits AICD cleavage to Aβ (IC50s = 531 and 131 nM for Aβ40 and Aβ42, respectively, in HeLa cell membranes); selective for AICD cleavage to Aβ over E-cadherin and Notch cleavage to E-cadherin γ-C-terminal fragments and NICD, respectively, at 30 µM; reduces cortical and hippocampal plaque area in Tg2576 mice at ~50 mg/kg per day; decreases plasma and brain Aβ40 and Aβ42 levels, as well as increases spontaneous alternations in the Y-maze in Tg2576 mice at 25 mg/kg per day

Formal name: N-(5-ethyl-2,4-dimethylphenyl)-4-[3-fluoro-4-(4-methyl-1H-imidazol-1-yl)phenyl]-2-thiazolamine

Synonyms: 

Molecular weight: 406.5

CAS: 1304630-27-0

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Neuroscience|Behavioral Neuroscience|Learning & Memory||Research Area|Neuroscience|Neurodegenerative Disorders|Alzheimer’s Disease

Related products

  • 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
    Add to quotes
    View product page
  • A zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 250 mg

    1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}  

     

    Brand:
    Cayman
    SKU:10009473 - 250 mg

    Available on backorder

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

    Anhydrotetracycline (hydrochloride) – 100 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 - 100 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page