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. MRK 560

    Catalog No. A15304
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    γ-secretase 抑制剂
    MRK 560是一种可用的γ-分泌酶抑制剂,能够显着减少大鼠脑和CSF中的Abeta肽,并证实该大鼠可用于评估γ-分泌酶抑制剂对中枢神经系统Abeta的作用(40)体内水平。 了解更多
  2. PF-03084014

    Catalog No. A11259
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    γ-secretase 抑制剂
    PF-03084014是一种可逆和选择性的γ-分泌酶抑制剂,IC50值为6.2 nM。 了解更多
  3. Flurbiprofen Axetil

    Catalog No. A13662
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    gamma-secretase 抑制剂
    Flurbiprofen Axetil是非甾体抗炎药(NSAID)。 了解更多
  4. L-685458

    Catalog No. A15899
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    γ-secretase 抑制剂
    L-685458是一种有效的A beta PPγ-分泌酶抑制剂,Ki为17 nM。 了解更多
  5. Begacestat (GSI-953)

    Catalog No. A11258
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    γ-secretase 抑制剂
    Begacestat (GSI-953)是一种新型的选择性淀粉样前体蛋白γ-分泌酶的噻吩磺酰胺抑制剂。 了解更多
  6. Verubecestat (MK-8931)

    Catalog No. A16113
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    β-secretase/BACE1 抑制剂
    Verubecestat (MK-8931)是一种有效的选择性β-分泌酶抑制剂,是BACE1蛋白抑制剂或Beta-site APP裂解酶1抑制剂。 了解更多
  7. Z-Ile-Leu-aldehyde

    Catalog No. A16215
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    γ-Secretase 抑制剂
    Z-Ile-Leu-aldehyde是一种有效的γ-分泌酶抑制剂;Notch信号抑制剂。 了解更多
  8. 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. 了解更多
  9. 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. 了解更多
  10. 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. 了解更多
  11. 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. 了解更多
  12. 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. 了解更多
  13. 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. 了解更多
  14. Compound E

    Catalog No. A21292
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    γ-secretase inhibitor
    Compound E is a γ-secretase inhibitor. 了解更多
  15. 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. 了解更多
  16. 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. 了解更多
  17. JLK 6

    Catalog No. A15301
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    γ-secretase 抑制剂
    JLK 6是γ-分泌酶的抑制剂,可选择性抑制APP裂解而不影响其他γ-分泌酶介导的途径。 了解更多
  18. Timosaponin b-II

    Catalog No. A14591
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    BACE1 抑制剂
    Timosaponin B-II是知母草(Liliaceae,根茎)的主要活性成分,对脑缺血性损伤具有保护作用。 了解更多
  19. AMG-8718

    Catalog No. A14407
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    BACE1 抑制剂
    AMG-8718是一种有效的BACE1抑制剂。 了解更多
  20. LY2886721

    Catalog No. A10543
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    BACE1 抑制剂
    LY2886721是一种有效的,选择性的,口服活性的β位淀粉样蛋白前体蛋白裂解酶 1 (BACE1) 抑制剂。LY2886721是一种新型强效药物,用于治疗阿尔茨海默病的研究。 了解更多
  21. AZD3839

    Catalog No. A12825
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    BACE1 抑制剂
    AZD3839是人类BACE1的有效选择性抑制剂,Ki为26.1 nM。 了解更多
  22. RO4929097

    Catalog No. A10802
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    Gamma-secretase 抑制剂
    RO4929097是一种γ secretase抑制剂,无细胞试验中IC50为4 nM。抑制Aβ40和Notch的细胞加工,EC50分别为14 nM和5 nM。 了解更多
  23. BMS-708163 (Avagacestat)

    Catalog No. A10157
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    Gamma-secretase 抑制剂
    BMS-708163 (Avagacestat)是口服生物有效的,选择性的γ-分泌酶抑制剂,作用于Aβ40和Aβ42时,IC50分别为0.3 nM和0.27 nM。 了解更多
  24. MK-0752

    Catalog No. A11194
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    Gamma-secretase 抑制剂
    MK-0752抑制Notch信号通路,这可能会导致Notch信号通路被过度激活的肿瘤细胞诱导生长停滞和凋亡。 了解更多
  25. DAPT (GSI-IX)

    Catalog No. A10288
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    Gamma secretase 抑制剂
    DAPT (GSI-IX)是一种γ-分泌酶抑制剂,可导致人原代神经元培养物中Aβ40和Aβ42水平降低,总Aβ和Aβ42的IC50值分别为115和200 nM。 了解更多
  26. YO-01027

    Catalog No. A11174
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    γ-secretase 抑制剂
    YO-01027是一种二肽γ-secretase抑制剂,作用于APPL和Notch分裂, 无细胞试验中IC50分别为2.6 nM和2.9 nM,一种抗阿尔茨海默氏病药物。 了解更多
  27. LY-411575

    Catalog No. A11176
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    Gamma secretase 抑制剂
    LY-411575是一种选择性的,细胞可渗透的小分子γ-secretase抑制剂。在表达APP或NΔE的HEK293细胞中IC50为0.078 nM/0.082 nM(基于膜/细胞),也抑制Notch分裂,IC50为0.39 nM。 了解更多
  28. Semagacestat (LY450139)

    Catalog No. A10836
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    Gamma-secretase 抑制剂
    Semagacestat (LY450139)是一种针对Aβ42,Aβ40和Aβ38的γ-分泌酶阻滞剂,IC50分别为10.9 nM,12.1 nM和12.0 nM。 Semagacestat还抑制Notch信号传导,IC50为14.1 nM。 了解更多
  29. LY2811376

    Catalog No. A11776
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    BACE1 抑制剂
    LY2811376是第一种可口服的非肽类BACE1抑制剂,可在动物体内产生显着的Aβ降低作用。 了解更多
  30. IMR-1A

    Catalog No. A16223
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    Notch 抑制剂
    IMR-1A是IMR-1的代谢产物。IMR-1是一类新型的Notch抑制剂,靶向转录激活,IC50为6 umol/L。 了解更多
  31. BMS 433796

    Catalog No. A11337
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    γ-Secretase 抑制剂
    BMS 433796是在阿尔茨海默病转基因小鼠模型中具有Aβ降低活性的γ分泌酶抑制剂。 了解更多
  32. IMR-1

    Catalog No. A16152
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    Notch 抑制剂
    IMR-1是一类新型的Notch抑制剂,靶向转录激活,IC50为6 umol/L。 了解更多
  33. BMS 299897

    Catalog No. A12444
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    γ-secretase 抑制剂
    BMS 299897是一种有效的γ-分泌酶抑制剂(IC50 = 12 nM)。在体外抑制Aβ40和Aβ42的形成(IC50值分别为7.4和7.9 nM),并在体内降低脑,血浆和脑脊髓液中的Aβ。 了解更多
  34. LY-900009

    Catalog No. A14088
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    Notch 抑制剂
    LY-900009是一种有效的Notch抑制剂,IC50值为0.27 nM。 了解更多
  35. FLI-06

    Catalog No. A13815
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    Gamma-secretase 抑制剂
    FLI-06是一种Notch抑制剂和早期分泌途径抑制剂。FLI-06以不同于布雷菲德菌素A和杀真菌剂A的方式破坏高尔基体。 了解更多
  36. LY3039478

    Catalog No. A13544
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    Notch 抑制剂
    LY3039478是一种新型小分子Notch抑制剂,在大多数测试的肿瘤细胞系中,IC50约为1nM。 了解更多

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