γ-Secretase

Catalog No.Inhibitor Name γ secretaseNotchOther
A10288DAPT (GSI-IX)
*
A10802RO4929097
***
***
Aβ40
A10836Semagacestat
**
**
A10157Avagacestat
****
A11174Dibenzazepine
***
***
A11176LY411575
****
****
A15899L-685458
*
A13815FLI-06
*
A13319PF-03084014
**
A11194MK-0752
***
Aβ40
A13544LY3039478
****
A16152IMR-1
*
A16223IMR-1A
*
A11258Begacestat (GSI-953)
**
A12444BMS 299897
A13217TC-E 5006
*
A15304MRK 560
****
A15301JLK 6
A16214CHF5074
*
A16215Z-Ile-Leu-aldehyde

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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  1. Z-Ile-Leu-aldehyde

    Catalog No. A16215
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    γ-Secretase inhibitor
    Z-Ile-Leu-aldehyde is a potent gamma-Secretase inhibitor; Notch signaling inhibitor. Learn More
  2. MRK 560

    Catalog No. A15304
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    γ-secretase inhibitor
    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. Learn More
  3. PF-03084014

    Catalog No. A11259
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    γ-secretase inhibitor
    PF-03084014 is a reversible and selective inhibitor of γ-secretase with IC50 value of 6.2 nM . Learn More
  4. L-685458

    Catalog No. A15899
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    γ-secretase inhibitor
    L-685458 is a specific and potent inhibitor of A beta PP gamma-secretase activity with Ki of 17 nM. Learn More
  5. Begacestat (GSI-953)

    Catalog No. A11258
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    γ-secretase inhibitor
    Begacestat is a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease. Learn More
  6. gamma-secretase modulator 1

    Catalog No. A11425
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    Gamma-secretase modulator
    gamma-secretase modulator 1 is a gamma-secretase modulator, gamma-secretase modulator 1 is useful for Alzheimer's disease. Learn More
  7. gamma-secretase modulator 2

    Catalog No. A11427
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    Gamma-secretase modulator
    gamma-secretase modulator 2 is a potent and selective gamma-secretase modulator for treatment of Alzheimer's disease. Learn More
  8. TC-E 5006

    Catalog No. A13217
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    Gamma-secretase modulator
    TC-E 5006 is a gamma-secretase modulator. Reduces Aβ42 levels in vitro (EC50 = 390 nM) and in vivo. Learn More
  9. Verubecestat (MK-8931)

    Catalog No. A16113
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    β-secretase/BACE1 inhibitor
    Verubecesta is a potent and selective beta-secretase inhibitor, and BACE1 protein inhibitor or Beta-site APP-cleaving enzyme 1 inhibitor. Learn More
  10. CHF5074

    Catalog No. A16214
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    γ-Secretase modulator
    CHF5074 is a novel γ-secretase modulator, reduces Aβ42 and Aβ40 secretion, with an IC50 of 3.6 and 18.4 uM, respectively. Learn More
  11. Flurbiprofen Axetil

    Catalog No. A13662
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    gamma-secretase inhibitor
    Flurbiprofen Axetil is potentnon-steroidal anti-inflammatory drug(NSAID). Learn More
  12. BACE1-IN-4

    Catalog No. A18462
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    BACE1 inhibitor
    BACE1-IN-4 is a potent and highly selective BACE1 inhibitor, with an IC50 of 3.8 nM and a Ki of 1.9 nM, more selective at BACE1 over BACE2. Anti-Alzheimer's disease. Learn More
  13. PF-06751979

    Catalog No. A20066
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    BACE1 inhibitor
    PF-06751979 is a potent, brain penetrant, β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 7.3 nM in BACE1 binding assay. Learn More
  14. Umibecestat (CNP520)

    Catalog No. A18987
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    BACE-1 inhibitor
    Umibecestat (CNP520) is a beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1) inhibitor with IC50s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively. Learn More
  15. Lanabecestat

    Catalog No. A12282
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    BACE1 inhibitor
    Lanabecestat (AZD3293) is a potent, highly permeable, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM. Learn More
  16. BACE1-IN-1

    Catalog No. A12183
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    BACE1 inhibitor
    BACE1-IN-1 is a potent and highly brain penetrant BACE1 inhibitor with IC50s of 32 and 47 nM for human BACE1 and BACE2, respectively. Learn More
  17. BMS-906024

    Catalog No. A21172
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    gamma secretase inhibitor
    BMS-906024 is an oral and selective gamma secretase inhibitor (GSI) that is a small molecule Notch inhibitor. Learn More
  18. Compound E

    Catalog No. A21292
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    γ-secretase inhibitor
    Compound E is a γ-secretase inhibitor. Learn More
  19. β-Secretase Inhibitor IV

    Catalog No. A21346
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    BACE-1 inhibitor
    β-Secretase Inhibitor IV is a potent, cell-active BACE-1 inhibitor with IC50s of 15.6 and 16.3nM under BACE-1 concentrations of 2 nM and 100 pM, respectively. Learn More
  20. AZD3839 free base

    Catalog No. A21606
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    BACE1 inhibitor
    AZD3839 (free base) is a potent and selective BACE1 inhibitor with IC50 of 23.6 uM, about 14-fold selectivity over BACE2, also a β-secretase enzyme inhibitor. Learn More
  21. Compound W

    Catalog No. A15296
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    Gamma-secretase modulator
    Compound W is a γ-secretase inhibitor that has been shown to lower the levels of secreted Aβ42 and Nβ25. Learn More
  22. LY2886721

    Catalog No. A10543
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    BACE1 inhibitor
    LY2886721 is a novel potent agent that is used to treat Alzheimer's Disease in preclinical experiments. Learn More
  23. AZD3839

    Catalog No. A12825
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    BACE1 inhibitor
    AZD3839 is a potent and selective inhibitor of human BACE1 with Ki of 26.1 nM. Learn More
  24. AMG-8718

    Catalog No. A14407
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    BACE1 inhibitor
    AMG-8718 is a potent and orally efficacious BACE1 inhibitor. Learn More
  25. JLK 6

    Catalog No. A15301
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    γ-secretase inhibitor
    JLK 6 is an inhibitor of γ-secretase that selectively inhibits APP cleavage without affecting other γ-secretase-mediated pathways. Learn More
  26. gamma-secretase modulator 3

    Catalog No. A15090
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    gamma-secretase modulator
    gamma-secretase modulator 3 is a gamma-secretase modulator. Learn More
  27. Timosaponin b-II

    Catalog No. A14591
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    BACE1 Inhibitor
    Timosaponin B-II is a major active component of Anemarrhena asphodeloides Bunge (Liliaceae, rhizome) that has protective effects against cerebral ischaemic damage. Learn More
  28. NGP-555

    Catalog No. A17051
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    γ-Secretase Modulator
    NGP-555 is a gamma-secretase modulator with a selective mechanism to reduce Abeta 42 while raising shorter Abeta forms such as Abeta 37 and 38. Learn More
  29. BMS-708163 (Avagacestat)

    Catalog No. A10157
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    Gamma-secretase inhibitor
    BMS-708163 is an oral gamma secretase inhibitor designed for selective inhibition of amyloid beta synthesis. Learn More
  30. MK-0752

    Catalog No. A11194
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    Gamma-secretase inhibitor
    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. Learn More
  31. DAPT (GSI-IX)

    Catalog No. A10288
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    Gamma secretase inhibitor
    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. Learn More
  32. YO-01027

    Catalog No. A11174
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    γ-secretase inhibitor
    YO-01027 is a dipeptidic γ-secretase inhibitor, an antiAlzheimer agent. Learn More
  33. LY-411575

    Catalog No. A11176
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    Gamma secretase inhibitor

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

    Learn More
  34. Semagacestat (LY450139)

    Catalog No. A10836
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    Gamma-secretase inhibitor
    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. Learn More
  35. LY2811376

    Catalog No. A11776
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    BACE1 inhibitor
    LY2811376 is the first orally available non-peptidic BACE1 inhibitor that produces profound Aβ-lowering effects in animals. Learn More
  36. BMS 433796

    Catalog No. A11337
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    γ-Secretase Inhibitor
    BMS 433796 is a γ-secretase inhibitor with Aβ lowering activity in a transgenic mouse model of Alzheimer's disease. Learn More
  37. BPN-15606

    Catalog No. A18681
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    γ-secretase modulator
    BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. Learn More
  38. IMR-1A

    Catalog No. A16223
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    Notch inhibitor
    IMR-1A is the metabolite of IMR-1. IMR-1 is a novel class of Notch inhibitors targeting the transcriptional activation with IC50 of 6 umol/L. Learn More
  39. E 2012

    Catalog No. A11393
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    gamma-secretase modulator
    E 2012 is γ-secretase inhibitor. Learn More
  40. BMS 299897

    Catalog No. A12444
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    γ-secretase inhibitor
    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. Learn More
  41. IMR-1

    Catalog No. A16152
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    Notch inhibitor
    IMR-1 is a novel class of Notch inhibitors targeting the transcriptional activation with IC50 of 6 umol/L. Learn More
  42. LY-900009

    Catalog No. A14088
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    Notch inhibitor
    LY-900009 is a potent inhibitor of Notch with IC50 value of 0.27 nM. Learn More
  43. Flurizan

    Catalog No. A12433
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    gamma-secretase modulator
    Flurizan is a nonsteroidal anti-inflammatory drug (NSAID) that inhibits γ-secretase activity. Learn More
  44. FLI-06

    Catalog No. A13815
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    Gamma-secretase inhibitor
    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. Learn More
  45. RO4929097

    Catalog No. A10802
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    Gamma-secretase inhibitor
    RO4929097 is an orally bioavailable, small-molecule gamma secretase (GS) inhibitor with an IC50 of 4 nM. Learn More
  46. LY3039478

    Catalog No. A13544
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    Notch inhibitor
    LY3039478 is a orally bioavailable, novel small molecule Notch inhibitor with an IC50 of ~1nM in most of the tumor cell lines tested. Learn More

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