γ-Secretase

γ-Secretase inhibitors and modulators act on the intramembrane protease that cleaves amyloid precursor protein (APP). The enzyme is a multiprotein complex with presenilin as its catalytic subunit, and Notch receptors are among its substrates. In 1998, loss of presenilin-1 in neurons was shown to block the γ-secretase cleavage of APP that releases amyloid-β (Aβ). A year later, a presenilin-1-dependent protease was found to release the Notch intracellular domain. DAPT, LY-411575 and semagacestat inhibit both APP and Notch processing and are used in Aβ and Notch signaling studies. Avagacestat and RO4929097 are further inhibitors, and DAPT is also common in organoid and stem cell work. E 2012 is a γ-secretase modulator that shifts Aβ production.

Items 1-25 of 82

  • LY-411575
    Cat. No.
    A11176

    LY-411575

    LY-411575 is a selective, cell permeable, small molecule gamma secretase inhibitor.

    2 mg
    $30.00
    5 mg
    $55.00
    All 7 sizes
  • DAPT
    Cat. No.
    A10288

    DAPT (GSI-IX)

    Synonyms: GSIIX

    DAPT (GSI-IX) is an inhibitor of γ-secretase that causes a reduction in Aβ40 and Aβ42 levels in human primary neuronal cultures with IC50 values of 115 and 200 nM for total Aβ and Aβ42 respectively.

    5 mg
    $35.00
    10 mg
    $65.00
    All 8 sizes
  • RO4929097
    Cat. No.
    A10802

    RO4929097

    RO4929097 is an orally bioavailable, small-molecule gamma secretase (GS) inhibitor with an IC50 of 4 nM.

    1 mg
    $35.00
    2 mg
    $50.00
    All 9 sizes
  • Semagacestat
    Cat. No.
    A10836

    Semagacestat (LY450139)

    Synonyms: LY-450139

    Semagacestat (LY450139) is a γ-secretase blocker for Aβ42, Aβ40 and Aβ38 with IC50 of 10.9 nM, 12.1 nM and 12.0 nM, respectively. Semagacestat also inhibits Notch signaling with IC50 of 14.1 nM.

    2 mg
    $25.00
    5 mg
    $45.00
    All 7 sizes
  • YO-01027
    Cat. No.
    A11174

    YO-01027

    Synonyms: Dibenzazepine; Deshydroxy LY 411575

    YO-01027 is a dipeptidic γ-secretase inhibitor, an antiAlzheimer agent.

    1 mg
    $35.00
    2 mg
    $55.00
    All 8 sizes
  • BMS 299897
    Cat. No.
    A12444

    BMS 299897

    BMS 299897 is an orally active, potent γ-secretase inhibitor (IC50 = 12 nM). Inhibits Aβ40 and Aβ42 formation in vitro (IC50 values are 7.4 and 7.9 nM respectively) and reduces Aβ in the brain, plasma and cerebrospinal fluid in vivo.

    5 mg
    $45.00
    10 mg
    $85.00
    All 6 sizes
  • FLI-06
    Cat. No.
    A13815

    FLI-06

    FLI-06 is a Notch inhibitor and the early secretory pathway inhibitor. FLI-06 disrupts the Golgi apparatus in a manner distinct from that of brefeldin A and golgicide A.

    1 mg
    $25.00
    2 mg
    $35.00
    All 9 sizes
  • MK-0752
    Cat. No.
    A11194

    MK-0752

    MK-0752 inhibits the Notch signaling pathway, which may result in induction of growth arrest and apoptosis in tumor cells in which the Notch signaling pathway is overactivated.

    1 mg
    $45.00
    5 mg
    $145.00
    All 7 sizes
  • Begacestat
    Cat. No.
    A11258

    Begacestat (GSI-953)

    Synonyms: GSI953

    Begacestat is a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease.

    2 mg
    $80.00
    5 mg
    $115.00
    All 6 sizes
  • BMS 433796
    Cat. No.
    A11337

    BMS 433796

    BMS 433796 is a γ-secretase inhibitor with Aβ lowering activity in a transgenic mouse model of Alzheimer's disease.

    1 mg
    $680.00
    5 mg
    $2,400.00
    All 2 sizes
  • Flurizan
    Cat. No.
    A12433

    Flurizan

    Synonyms: (R)-Flurbiprofen; MPC 7869; Tarenflurbil

    Flurizan is a nonsteroidal anti-inflammatory drug (NSAID) that inhibits γ-secretase activity.

    100 mg
    $45.00
    250 mg
    $105.00
    All 4 sizes
  • TC-E 5006
    Cat. No.
    A13217

    TC-E 5006

    TC-E 5006 is a gamma-secretase modulator. Reduces Aβ42 levels in vitro (EC50 = 390 nM) and in vivo.

    5 mg
    $520.00
    10 mg
    $920.00
    All 4 sizes
  • SPL-707
    Cat. No.
    A13669

    SPL-707

    SPL-707 is a potent, selective and orally available signal peptide peptidase-like 2a (SPPL2a) inhibitor with an IC50 of 80 nM.

    1 mg
    $315.00
    5 mg
    $775.00
    All 3 sizes
  • Compound W
    Cat. No.
    A15296

    Compound W

    Synonyms: CW3,5-Bis(4-nitrophenoxy)benzoic acid

    Compound W is a γ-secretase inhibitor that has been shown to lower the levels of secreted Aβ42 and Nβ25.

    5 mg
    $20.00
    10 mg
    $25.00
    All 6 sizes
  • JLK 6
    Cat. No.
    A15301

    JLK 6

    JLK 6 is an inhibitor of γ-secretase that selectively inhibits APP cleavage without affecting other γ-secretase-mediated pathways.

    1 mg
    $125.00
    5 mg
    $265.00
    All 8 sizes
  • MRK 560
    Cat. No.
    A15304

    MRK 560

    MRK 560 is an orally bioavailable gamma-secretase inhibitor with the ability to markedly reduce Abeta peptide in the brain and CSF of the rat and confirm the utility of the rat for assessing the effects of gamma-secretase inhibitors on central nervous system Abeta(40) levels in vivo.

    2 mg
    $30.00
    5 mg
    $50.00
    All 7 sizes
  • L-685458
    Cat. No.
    A15899

    L-685458

    Synonyms: L685,458

    L-685458 is a specific and potent inhibitor of A beta PP gamma-secretase activity with Ki of 17 nM.

    1 mg
    $115.00
    2 mg
    $215.00
    All 8 sizes
  • Verubecestat
    Cat. No.
    A16113

    Verubecestat (MK-8931)

    Synonyms: MK-8931

    Verubecesta is a potent and selective beta-secretase inhibitor, and BACE1 protein inhibitor or Beta-site APP-cleaving enzyme 1 inhibitor.

    2 mg
    $25.00
    5 mg
    $50.00
    All 8 sizes

Items 1-25 of 82

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