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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.

Items 1-10 of 18

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  1. TC-E 5006
    Catalog No. :
    B7719
    γ-secretase modulator
    New Product
  2. Begacestat
    Catalog No. :
    A4406
    γ-secretase inhibitor
    γ-secretase inhibitor; selectively inhibits cleavage of amyloid precursor protein (APP) over Notch.
  3. Flurizan
    Catalog No. :
    A4402
    NSAID,inhibits γ-secretase activity
    Nonsteroidal anti-inflammatory drug (NSAID) that inhibits γ-secretase activity.
  4. MRK 560
    Catalog No. :
    A4405
    γ-secretase inhibitor
    γ-secretase inhibitor; inhibits proteolytic cleavage of amyloid precursor protein (APP) over the Notch pathway. Reduces levels of Aβ in the brain (inhibits Aβ40 and Aβ42 in SH-SY5Y neuroblastoma cells with an IC50 of 0.65 nM); attenuates plaque deposition. Orally bioavailable.
  5. L-685,458
    Catalog No. :
    A4404
    γ-secretase inhibitor

    L-685,458 is a selective and Potent inhibitor of γ-secretase with IC50 value of 17 nM.

  6. JLK 6
    Catalog No. :
    A4403
    γ-secretase inhibitor
    Inhibitor of γ-secretase that selectively inhibits βAPP cleavage without affecting other γ-secretase-mediated pathways. Prevents recovery of Aβ40 and Aβ42 from HEK293 cell overexpressing wild-type or Swedish-mutated βAPP (IC50 ~ 30 μM) but displays no effect on Notch cleavage and Notch-mediated intracellular signaling. Displays no activity on BACE1, BACE2, α-secretase, the proteosome or GSK3β.
  7. Compound W
    Catalog No. :
    A4401
    γ-secretase inhibitor
    Inhibitor of γ-secretase; causes a decrease in the released levels of Aβ42 and notch-1 Aβ-like peptide 25 (Nβ25).
  8. BMS 299897
    Catalog No. :
    A4400
    γ--secretase inhibitor, potent and orally active
    BMS-299897 is a selective inhibitor of γ-secretase with IC50 value of 12 nM [1].
  9. PF-03084014
    Catalog No. :
    A3711
    γ-secretase inhibitor
    PF-03084014 is a reversible and selective inhibitor of γ-secretase with IC50 value of 6.2 nM .
  10. LY3039478
    Catalog No. :
    A4023
    Notch inhibitor, novel and potent

    LY3039478 is a novel and potent Notch inhibitor with IC50 of 0.41 nM.

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