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Gamma Secretase

Gamma secretase (γ-secretase), a member of the intramembrane cleaving protease (i-CLiP) family, is a promiscuous di-aspartyl protease that catalyzes the regulated intramembrane proteolysis (RIP), in which substrate proteins are cleaved within their membrane-spanning domain. A functional γ-secretase is a multi-protein complex consisting of the catalytic component, presenilin (PSEN), and three protein cofactors, including nicastrin (NCT), anterior-pharynx defective-1 (APH1) and PSEN enhancer-2 (PEN2). So far, 90 substrates of γ-secretase have been identified, which are type-I transmembrane proteins, except for glutamate receptor GluR3, polycystin-1 and glucosaminyltransferase (GnT-V), and appear to function as signaling proteins regulating a wide variety of cellular events, such as Notch signaling pathway.

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  1. Cat.No. Product Name Information
  2. A4022 BMS-708163 (Avagacestat) BMS-708163 is a potent selective and orally bioavailable inhibitor of γ-secretase with IC50 value of 0.3nM .
  3. A8200 DAPT (GSI-IX) DAPT (GSI-IX) is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells.
  4. A3427 gamma-secretase modulator 3 gamma-secretase modulator 3 is a gamma-secretase modulator.
  5. A3426 gamma-secretase modulator 2 gamma-secretase modulator is modulation of the action of γ-secretase so as to Selectively attenuate production of Aβ(1-42) and hence find use in treatment or prevention of diseases associated with deposition of Aβ in the brain.
  6. A3425 gamma-secretase modulator 1 gamma-secretase inhibitior-1 is useful for Alzheimer's disease.
  7. A4005 RO4929097 RO4929097 is a small-molecule inhibitor of γ secretase with IC50 of 4 nM and EC50 of 5 nM.
  8. A8190 Semagacestat (LY450139) Semagacestat (also known as LY450139), [(2S)-2-hydroxy-N-((2S)-1-((1S)-3-methyl-2-oxo-2,3,4,5-tetrahydro-1H-benzo[d]azepin-1ylamino)-1-oxopropan-2-yl)-3-methylbutanamide] is an azepine class γ-secretase, which is currently being investigated as a potential disease-modifying agent for the treatment of Alzheimer’s disease (AD).
  9. A4006 MK-0752 MK-0752 is a potent gamma secretase inhibitor in clinical development (IC50 ~50 nM). Gamma secretase is an important component in the NOTCH cleavage machinery that catalyzes the cleavage of receptor protein substrates within their transmembrane domain. Inhibition of Notch inhibits BC cell proliferation in vitro.
  10. A4018 YO-01027 (Dibenzazepine, DBZ)

    YO-01027, also known as dibenzazepine or DBZ, is a potent inhibitor of γ-secretase, a multisubunit aspartyl protease catalyzing the cleavage of numerous type I integral membrane proteins (such as amyloid precursor protein (APP) and Notch).

  11. A4019 LY-411575 LY-411575 is a potent inhibitor of γ-secretase with IC50 value of 0.078 nM in membrane assay.

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