1. Neuronal Signaling
    Stem Cell/Wnt
  2. γ-secretase

γ-secretase

The γ-secretases are intramembrane cleaving protein complexes responsible for the generation of amyloid β (Aβ) from the amyloid precursor protein (APP). Apart from presenilins (PSEN) , a mature and active γ-secretase complex consists of three additional subunits: Nicastrin (Nct), PSEN enhancer 2 (Pen-2), and either anterior pharynx 1 (APH-1) A or B. The γ-secretase complexes proteolyse type 1 transmembrane proteins, among them the APP, the Notch receptors and ligands, the Erb4 receptor and N-Cadherin.

Inhibition of γ-secretase with DAPT significantly reduced the production of extracellular Aβ38, Aβ40, and Aβ42 in neurons of all genotypes.

Compounds that inhibit or modulate γ-secretase can be considered as a potential therapeutics for AD because their use appears to be a rational strategy to prevent senile plaque (SP) formations.

γ-secretase Related Products (19):

Cat. No. Product Name Effect Purity
  • HY-13027
    DAPT Inhibitor 99.25%
    DAPT is a γ-secretase inhibitor, reduces the total beta-amyloid peptide () production with IC50 of 20 nM in HEK 293 cells.
  • HY-11102
    RO4929097 Inhibitor 98.02%
    RO4929097 is a γ secretase inhibitor with IC50 of 4 nM, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively.
  • HY-15185
    PF-3084014 Inhibitor 98.03%
    PF-3084014 is a reversible, noncompetitive, and selective γ-secretase inhibitor with IC50 of 6.2 nM.
  • HY-50845
    BMS-708163 Inhibitor 99.95%
    BMS-708163 is a potent inhibitor of γ-secretase, with IC50s of 0.27 nM and 0.30 nM for Aβ42 and Aβ40 inhibition; Also inhibits NICD (Notch IntraCellular Domain) with IC50 of 0.84 nM and shows weak inhibition of CYP2C19, with IC50 of 20 μM.
  • HY-10009
    Semagacestat Inhibitor 98.90%
    Semagacestat is a γ-secretase inhibitor, inhibits β-amyloid (Aβ42), Aβ38 and Aβ40 with IC50 of 10.9, 12 and 12.1 nM, respectively; also inhibits Notch signaling with IC50 of 14.1 nM.
  • HY-13526
    YO-01027 Inhibitor 98.22%
    YO-01027 (Dibenzazepine;DBZ) is a potent γ-secretase inhibitor with IC50 values of 2.92±0.22 and 2.64±0.30 nM for Notch and APPL cleavage, respectively.
  • HY-50883
    BMS 299897 Inhibitor 99.35%
    BMS 299897 is a sulfonamide γ-secretase inhibitor with an IC50 of 7 nM for Aβ production inhibition in HEK293 cells stably overexpressing amyloid precursor protein (APP).
  • HY-50752
    LY-411575 Inhibitor 99.22%
    LY-411575 is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), and also inhibits Notch S3 cleavage with IC50 of 0.39 nM.
  • HY-19369
    L-685458 Inhibitor 99.57%
    L-685458 is a potent inhibitor of Amyloid β-Protein precursor γ-secretase activity with IC50 of 17 nM, shows greater than 50-100-fold selectivity over other aspartyl proteases tested.
  • HY-10974
    MK-0752 Inhibitor 98.87%
    MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM.
  • HY-10016
    E 2012 Modulator
    E 2012 is a potent γ-secretase modulator.
  • HY-14399
    CHF5074 Inhibitor
    CHF5074 is a novel γ-secretase modulator, reduces Aβ42 and Aβ40 secretion, with an IC50 of 3.6 and 18.4 μM, respectively.
  • HY-50889
    gamma-secretase modulator 3 Modulator
    gamma-secretase modulator 3 is a gamma-secretase modulator.
  • HY-10043
    gamma-secretase modulator 1 Modulator >98.0%
    γ-secretase inhibitior-1 is a gamma-secretase modulator, γ-secretase inhibitior-1 is useful for Alzheimer's disease.
  • HY-12465
    Z-Ile-Leu-aldehyde Inhibitor
    Z-Ile-Leu-aldehyde(Z-IL-CHO; GSI-XII) is a potent gamma-Secretase inhibitor; Notch signaling inhibitor.
  • HY-50752B
    LY-411575 isomer 2
    LY-411575 isomer 2 is an isomer of LY411575, which is a potent γ-secretase inhibitor.
  • HY-50752A
    LY-411575 isomer 1
    LY-411575 isomer 1 is an isomer of LY411575, which is a potent γ-secretase inhibitor.
  • HY-50752C
    LY-411575 isomer 3
    LY-411575 isomer 3 is an isomer of LY411575, which is a potent γ-secretase inhibitor.
  • HY-50754
    gamma-secretase modulator 2 Modulator
    gamma-secretase modulator 2 is a potent and selective γ-secretase modulator for treatment of Alzheimer's disease.