A multimeric aspartyl protease called -Secretase breaks down the membrane-spanning portion of the -carboxyl terminal fragment (CTF) that results from -amyloid precursor protein. A crucial molecule in the pathogenesis of Alzheimer's disease (AD), -Secretase defines the generated molecular species of amyloid protein (A).
Secretase is made up of four subunits: presenilin (PS), the catalytic subunit of the enzyme, nicastrin (Nct), pen-2, and apha-1. In order to activate -secretase, PS must undergo endoproteolysis, which produces PS1-NTF (N-terminal fragment) and CTF (C-terminal fragment) heterodimer. Amyloid precursor protein (APP), Notch, and numerous other substrates are broken down by -Secretase. The pathogenesis of AD is influenced by abnormal APP cleavage, and abnormal Notch signaling encourages tumor growth. Secretase is a highly sought-after drug target in cancer and Alzheimer's disease. Both inhibitors (GSIs) and modulators (GSMs), two different classes of small molecules that target -secretase, have been created.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V94832 | (-)-FRM-024 | 2085780-85-2 | (-)-FRM-024 is the (-)-isomer of FRM-024, a potent, central nervous system-penetrating γ-secretase modulator for Alzheimer's disease research. |
|
V103302 | (9R)-RO7185876 | 2226077-86-5 | (9R)-RO7185876 (Compound Example 16) is a γ-secretase inhibitor. |
|
V67532 | 3,5-Bis(4-nitrophenoxy)benzoic acid | 173550-33-9 | 3,5-Bis(4-nitrophenoxy)benzoic acid is a gamma-secretase inhibitor. |
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V112043 | AZ1136 | 1380508-60-0 | AZ1136 is a highly selective γ-secretase regulator (GSM). |
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V67525 | Aβ42-IN-1 | 2582757-69-3 | Aβ42-IN-1, compound 1v, is a novel, potent and orally bioactive gamma-secretase modulator (GSM). |
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V67523 | Aβ42-IN-1 free base | 2434633-17-5 | Aβ42-IN-1 free base is an orally bioactive, high-exposure γ-secretase modulator. |
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V67519 | Aβ42-IN-2 | 1914989-80-2 | Aβ42-IN-2 is a γ-secretase modulator. |
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V115825 | BIIB042 | 1257396-73-8 | BIIB042 is a potent, orally effective, blood-brain barrier-crossing, selective γ-secretase (GSM) modulator. |
|
V67526 | BPN-15606 besylate | 2436239-00-6 | BPN-15606 besylate is a potent orally bioactive γ-secretase modulator (GSM) that attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50s of 7 nM and 17 nM respectively. |
|
V3549 | Compound E | 209986-17-4 | Compound E (ɣ-secretase inhibitor XXI) is a novel, potent, cell-permeable, and selective inhibitor of γ-secretase with potential anti-AD (Alzheimers disease) effects. |
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V3492 | BMS 299897 | 290315-45-6 | BMS 299897 is a novel and potent sulfonamideγ-secretaseinhibitor with anIC50of 7 nM for Aβ production inhibition in HEK293 cells stably overexpressing amyloid precursor protein (APP). |
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V67521 | Fosciclopirox (CPX-POM) | 1380539-06-9 | Fosciclopirox suppresses the growth of urothelial cancer by targeting gamma-secretase. |
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V85158 | Fosciclopirox disodium (CPX-POM disodium) | 1380539-08-1 | |
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V67528 | FRM-024 | 2085780-87-4 | FRM-024 is a potent CNS-permeable/penetrable gamma-secretase modulator and a candidate for familial Alzheimer's disease (AD). |
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V67520 | gamma-secretase modulator 1 hydrochloride | 2741571-83-3 | gamma-secretase inhibitor-1 is a gamma-secretase modulator that acts in Alzheimer's disease (AD). |
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V97420 | GSI-18 | 362653-62-1 | GSI-18 is a γ-secretase inhibitor with anticancer activity. |
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V67529 | LY-411575 (isomer 2) | 2070009-70-8 | LY-411575 isomer 2 is an enantiomer of LY411575, a effective inhibitor of γ-secretase. |
|
V67530 | LY-411575 (isomer 3) | 2070009-28-6 | LY-411575 isomer 3 is an enantiomer of LY411575, a effective inhibitor of γ-secretase. |
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V100246 | LY3056480 | 2064292-78-8 | LY3056480 is a γ-secretase inhibitor (GSI) that inhibits Notch signaling. |
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V93808 | Nivegacetor | 2443487-67-8 | Nivegacetor is a potent γ-secretase modulator. |
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