1. Signaling Pathways
  2. Neuronal Signaling
    Stem Cell/Wnt
  3. 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 (38):

Cat. No. Product Name Effect Purity
  • HY-13027
    DAPT Inhibitor 99.97%
    DAPT (GSI-IX) is a potent and orally active γ-secretase inhibitor with IC50s of 115 nM and 200 nM for total amyloid-β (Aβ) and 42, respectively. DAPT inhibits the activation of Notch 1 signaling and induces cell differentiation. DAPT also induces autophagy and apoptosis. DAPT has neuroprotection activity and has the potential for autoimmune and lymphoproliferative diseases, degenerative disease and cancers treatment.
  • HY-11102
    RO4929097 Inhibitor 98.29%
    RO4929097 (RG-4733) 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
    Nirogacestat Inhibitor 99.95%
    Nirogacestat (PF-3084014) is a reversible, noncompetitive, and selective γ-secretase inhibitor with IC50 of 6.2 nM.
  • HY-13526
    YO-01027 Inhibitor 99.23%
    YO-01027 (Dibenzazepine;DBZ) is a potent γ-secretase inhibitor with IC50 values of 2.92 and 2.64 nM for Notch and APPL cleavage, respectively.
  • HY-12449
    Crenigacestat Inhibitor 98.62%
    Crenigacestat is an orally active Notch and γ-secretase inhibitor, with an IC50 of ∼1nM in most of the tumor cell lines tested.
  • HY-50882
    ELN318463 Inhibitor
    ELN318463 is an amyloid precursor protein (APP) selective γ-secretase inhibitor. ELN318463 shows differential inhibition of presenilin (PS1)- and PS2-comprised γ-secretase with EC50s of 12 nM and 656 nM for PS1 and PS2, respectively. ELN318463 is 51-fold more selective for PS1.
  • HY-130609A
    Aβ42-IN-1 free base Modulator
    Aβ42-IN-1 free base (compound 1v) is an orally active, high brain exposure γ-secretase modulator. Aβ42-IN-1 free base potently reduces Aβ42 levels with an IC50 value of 0.091 µM, and significantly reduces brain Aβ42 levels in mice. Aβ42-IN-1 free base is a promising compound for the treatment of Alzheimer’s disease.
  • HY-120789
    PF-06648671 Modulator
    PF-06648671 is a novel, brain‐penetrable, and orally active γ‐secretase modulator (GSM). PF-06648671 reduces Aβ42 and Aβ40, with concomitant increases in Aβ37 and Aβ38 in vitro. PF-06648671 is used for the study of Alzheimer’s disease.
  • HY-50752
    LY-411575 Inhibitor 99.20%
    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-14176
    Compound E Inhibitor 99.87%
    Compound E is a γ-secretase inhibitor. Compound E bloks β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage with IC50s of 0.24, 0.37, 0.32 nM, respectively.
  • HY-10974
    MK-0752 Inhibitor 98.00%
    MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM.
  • HY-10009
    Semagacestat Inhibitor 98.83%
    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-19369
    L-685458 Inhibitor 99.78%
    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-14399
    Itanapraced Inhibitor >98.0%
    Itanapraced (CHF5074) is a novel γ-secretase modulator, reduces Aβ42 and Aβ40 secretion, with an IC50 of 3.6 and 18.4 μM, respectively.
  • HY-108714
    NGP555 Modulator 98.64%
    NGP555 is a γ-secretase modulator.
  • HY-10016
    E 2012 Modulator
    E 2012 is a potent gamma (γ) secretase modulator without affecting Notch processing. E 2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis. E 2012 aims at Alzheimer's disease by reduction of amyloid β-42, and induces cataract following repeated doses in the rat.
  • HY-50883
    BMS 299897 Inhibitor 98.96%
    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-50845
    Avagacestat Inhibitor
    Avagacestat (BMS-708163) is a potent inhibitor of γ-secretase, with IC50s of 0.27 nM and 0.30 nM for Aβ42 and Aβ40 inhibition; Avagacestat (BMS-708163) also inhibits NICD (Notch IntraCellular Domain) with IC50 of 0.84 nM and shows weak inhibition of CYP2C19, with IC50 of 20 μM.
  • HY-12465
    Z-Ile-Leu-aldehyde Inhibitor 98.10%
    Z-Ile-Leu-aldehyde (Z-IL-CHO) is a potent and competitive peptide aldehyde inhibitor of γ-secretase and notch.
  • HY-14174
    MRK-560 Inhibitor >99.0%
    MRK-560 is a potent, orally bioavailable and brain-penetrant γ-secretase inhibitor.
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