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
    PF-3084014 is a reversible, noncompetitive, and selective γ-secretase inhibitor with IC50 of 6.2 nM.
  • HY-50845
    BMS-708163 Inhibitor 99.95%
    Avagacestat (BMS-708163) is a potent, selective, orally bioavailable (gamma)-secretase inhibitor of A(beta)40 and A(beta)42 with IC50 of 0.3 nM and 0.27 nM, demonstrating a 193-fold selectivity against Notch.
  • HY-10009
    Semagacestat Inhibitor 98.9%
    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%
    LY411575 is a potent (gamma)-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), also inhibits Notch clevage with withIC50 of 0.39 nM.
  • HY-19369
    L-685458 Inhibitor 99.57%
    L-685458 is a potent inhibitor of Amyloid (beta)-Protein precursor (gamma)-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 (gamma)-secretase inhibitor, which reduces A(beta)40 production with IC50 of 5 nM.
  • HY-10016
    E 2012 Modulator
    E 2012 is a potent (gamma)-secretase modulator.
  • HY-14399
    CHF5074 Inhibitor 98.05%
    CHF5074 is a novel (gamma)-secretase modulator, reduces A(beta)42 and A(beta)40 secretion, with an IC50 of 3.6 and 18.4 (mu)M, 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%
    (gamma)-secretase inhibitior-1 is a gamma-secretase modulator, (gamma)-secretase inhibitior-1 is useful for Alzheimer(acute)s disease.
  • HY-12465
    Z-Ile-Leu-aldehyde Inhibitor 98.1%
    Z-Ile-Leu-aldehyde(Z-IL-CHO; GSI-XII) is a potent gamma-Secretase inhibitor; Notch signaling inhibitor.
  • HY-50754
    gamma-secretase modulator 2 Modulator
    gamma-secretase modulator 2 is a potent and selective (gamma)-secretase modulator for treatment of Alzheimer(acute)s disease.
  • HY-50752A
    LY-411575 isomer 1 Inhibitor 99.06%
    LY-411575 isomer 1 is a isomer of LY411575, which is a potent (gamma)-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), also inhibits Notch clevage with withIC50 of 0.39 nM.
  • HY-50752B
    LY-411575 isomer 2 Inhibitor
    LY-411575 isomer 2 is a isomer of LY411575, which is a potent (gamma)-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), also inhibits Notch clevage with withIC50 of 0.39 nM.
  • HY-50752C
    LY-411575 isomer 3 Inhibitor
    LY-411575 isomer 3 is a isomer of LY411575, which is a potent (gamma)-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), also inhibits Notch clevage with withIC50 of 0.39 nM.