γ-Secretase is a multimeric aspartyl protease that cleaves the membrane-spanning region of the β-carboxyl terminal fragment (βCTF) generated from β-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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V0718 | Avagacestat (BMS-708163) | 1146699-66-2 | Avagacestat (formerly known as BMS708163) is a potent, selective, orally bioactive γ -secretase inhibitor of Aβ40 and Aβ42 with potential anti-AD (Alzheimers disease) activity. |
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V0714 | DAPT (GSI-IX; LY374973) | 208255-80-5 | DAPT (also known as GSI-IX; LY-374973) is a novel, potent and selective γ-secretase inhibitor used in the study of the Notch signaling pathway and is reported to be able to reduce the levels of beta-amyloid in a mouse model of Alzheimer's disease. |
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V0722 | FLI-06 | 313967-18-9 | FLI-06 (FLI 06; FLI-06) is a novel and potent inhibitor of Notch signaling pathway with EC50 of 2.3 μM. |
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V0719 | L-685,458 | 292632-98-5 | L-685,458 (also called L685458; L-685458) is a selective inhibitor of Aß PP γ-secretase with potential anti-AD and anticancer activity. |
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V0721 | LY411575 (LY411575; LSN 411575) | 209984-57-6 | LY411575 (also named as LY-411575; LY 411575; LSN-411575; LSN411575) is a dibenzoazepine-based,cell permeable and selective Gamma/γ-secretase inhibitor with potential anti-AD ( Alzheimers disease) activity. |
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V0717 | MK-0752 | 471905-41-6 | MK0752 (MK0752; MK-0752) is a novel, potent and synthetic small molecule inhibitor of γ-secretase (gamma-secretase). |
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V0723 | Nirogacestat (PF-03084014; PF-3084014) | 1290543-63-3 | Nirogacestat (formerly also known as PF-03084014; PF03084014;PF 3084014; PF-3084014) is an orally bioavailable, reversible, noncompetitive, andselective γ-secretase/gamma secretase (GS) inhibitor with potential anticancer activity. |
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V0715 | RO4929097 (RO4929097; R4733; RO04929097) | 847925-91-1 | RO4929097 (also called RO-4929097; RO04929097; R-4733) is a novel, potent and orally bioavailable small molecule inhibitor of the γ-secretase (gamma secretase-GS) with potential antitumor activity. |
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V0716 | Semagacestat (LY-450139; LY-4501) | 425386-60-3 | Semagacestat (also known as LY450139; LY4501) is a novel and potent γ-secretase inhibitor/blocker for Aβ42, Aβ40 and Aβ38 with the potential for treating Alzheimer's disease. |
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V0720 | YO-01027 (Dibenzazepine; YO 01027) | 209984-56-5 | YO-01027 (also called dibenzazepine; DBZ; YO01027) is a novel, potent, orally bioavailable, dipeptidic inhibitor of the γ-secretase with potential antineoplastic activity. |
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