γ-secretase
Gamma secretase
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. γ-Secretase defines the generated molecular species of amyloid β-protein (Aβ), a critical molecule in the pathogenesis of Alzheimer's disease (AD).
γ-Secretase is composed of four subunits: Aph-1, nicastrin (Nct), Pen-2 and presenilin (PS), which is the catalytic subunit of the enzyme. Endoproteolysis of PS, which results in the formation of PS1-NTF (N-terminal fragment) and CTF (C-terminal fragment) heterodimer, is required for γ-secretase activation. γ-Secretase cleaves amyloid precursor protein (APP), Notch and many other substrates. Aberrant cleavage of APP contributes to the pathogenesis of AD and abnormal Notch signaling promotes tumor growth. γ-Secretase is a highly valued drug target in Alzheimer's disease and cancer. Multiple classes of small molecules that target γ-secretase have been developed, including both inhibitors (GSIs) and modulators (GSMs).
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γ-secretase Related Products (118)
Related Products (118)
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Antibodies (5)
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Avagacestat (Standard)
0 ImagesSynonyms: BMS-708163 (Standard)Avagacestat (Standard) is the analytical standard of Avagacestat. This product is intended for research and analytical applications. Avagacestat (BMS-708163) is a potent inhibitor of γ-secretase, with IC50s of 0.27 nM and 0.30 nM for Aβ42 and Aβ40 inhibition; Avagacestat (BMS-708163) also inhibits NICD (Notch IntraCellular Domain) with IC50 of 0.84 nM and shows weak inhibition of CYP2C19, with IC50 of 20 μM. Avagacestat can be used for Alzheimer disease research.
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YO-01027 (Standard)
0 ImagesCat. No.: HY-13526RCAS No.: 209984-56-5Synonyms: Dibenzazepine (Standard); DBZ (Standard)
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Bepridil hydrochloride (Standard)
0 ImagesSynonyms: CERM 1978 (Standard); Org 5730 hydrochloride (Standard)Bepridil hydrochloride (Standard) (CERM 1978 (Standard);Org 5730 hydrochloride (Standard)) is the analytical standard of Bepridil hydrochloride (HY-103315). This product is intended for research and analytical applications. Bepridil hydrochloride is an orally active non-selective calcium channel antagonist with multi-ion channel blocking activity. Bepridil hydrochloride modulates Calmodulin, the 20S proteasome, T-type/L-type calcium channels, cardiac sodium channels, multiple potassium channels, γ-secretase, β-secretase, and mitoKATP/sarcKATP channels. Bepridil hydrochloride acts as a hydroxyl radical scavenger, regulates mitochondrial and intracellular calcium handling, and exerts antiarrhythmic, antianginal, and cardioprotective effects. Bepridil hydrochloride alters amyloid precursor protein processing, reduces β-amyloid and thalamic calcium levels, restores seladin-1/DHCR24 expression, and improves sensorimotor recovery after cerebral ischemia. Bepridil hydrochloride also exhibits potent inhibitory effects on SARS-CoV-2 replication. Bepridil hydrochloride is used in studies related to stable angina, arrhythmias, cerebral ischemia, Alzheimer's disease, and SARS-CoV-2 infection.
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E 2012 (Standard)
0 ImagesCat. No.: HY-10016RCAS No.: 870843-42-8E 2012 (Standard) is the analytical standard of E 2012 (HY-10016). This product is intended for research and analytical applications. E 2012 is a potent gamma (γ) secretase modulator without affecting Notch processing. E 2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis. E 2012 aims at Alzheimer's disease by reduction of amyloid β-42, and induces cataract following repeated doses in the rat.
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Bepridil-d5 hydrochloride
0 ImagesCat. No.: HY-103315SSynonyms: CERM 1978-d5; Org 5730-d5 hydrochlorideBepridil-d5 hydrochloride (CERM 1978-d5; Org 5730-d5 hydrochloride) is the deuterated-labeled Bepridil hydrochloride (HY-103315). Bepridil hydrochloride (CERM 1978; Org 5730 hydrochloride) is an orally active non-selective calcium channel antagonist with multi-ion channel blocking activity. Bepridil hydrochloride modulates Calmodulin, the 20S proteasome, T-type/L-type calcium channels, cardiac sodium channels, multiple potassium channels, γ-secretase, β-secretase, and mitoKATP/sarcKATP channels. Bepridil hydrochloride acts as a hydroxyl radical scavenger, regulates mitochondrial and intracellular calcium handling, and exerts antiarrhythmic, antianginal, and cardioprotective effects. Bepridil hydrochloride alters amyloid precursor protein processing, reduces β-amyloid and thalamic calcium levels, restores seladin-1/DHCR24 expression, and improves sensorimotor recovery after cerebral ischemia. Bepridil hydrochloride also exhibits potent inhibitory effects on SARS-CoV-2 replication. Bepridil hydrochloride is used in studies related to stable angina, arrhythmias, cerebral ischemia, Alzheimer's disease, and SARS-CoV-2 infection.
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MK-0752 (Standard)
0 ImagesCat. No.: HY-10974RCAS No.: 471905-41-6MK-0752 (Standard) is the analytical standard of MK-0752 (HY-10974). This product is intended for research and analytical applications. MK-0752 is a potent, orally active and specific γ-secretase inhibitor, showing dose-dependent reduction of Aβ40 with an IC50 of 5 nM in human SH-SY5Y cells. MK-0752 crosses the blood-brain barrier. MK-0752 reduces newly generated CNS Aβ in vivo.
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Begacestat (Standard)
0 ImagesCat. No.: HY-14175RCAS No.: 769169-27-9Synonyms: GSI-953 (Standard)Begacestat (Standard) is the analytical standard of Begacestat. This product is intended for research and analytical applications. Begacestat (GSI-953) is a selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase (IC50Aβ40=15 nM) for the treatment of Alzheimer's disease.
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LY-411575 (isomer 1)
0 ImagesLY-411575 isomer 1 is an isomer of LY411575, which is a potent γ-secretase inhibitor.
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RO4929097 (Standard)
0 ImagesCat. No.: HY-11102RCAS No.: 847925-91-1Synonyms: RG-4733 (Standard)RO4929097 (Standard) is the analytical standard of RO4929097 (HY-11102). This product is intended for research and analytical applications. RO4929097 (RG-4733) is an orally active γ secretase inhibitor with an IC50 of 4 nM, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively.
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PSEN1-IN-1
0 ImagesCat. No.: HY-156011CAS No.: 3054220-62-8PSEN1-IN-1 (Compound (+)-13b) is a PSEN1 inhibitor. PSEN1-IN-1 inhibits PSEN1-APH1A and PSEN1-APH1B complex with IC50s of 19 and 5.5 nM. PSEN1-IN-1 can be used for Alzheimer's disease research.
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Semagacestat (Standard)
0 ImagesSynonyms: LY450139 (Standard)Semagacestat (Standard) is the analytical standard of Semagacestat. This product is intended for research and analytical applications. Semagacestat is a γ-secretase inhibitor, inhibits β-amyloid (Aβ42), Aβ38 and Aβ40 with IC50s of 10.9, 12 and 12.1 nM, respectively; also inhibits Notch signaling with IC50 of 14.1 nM. Semagacestat can be used for the research of alzheimer's?disease.
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SPL-707 (Standard)
0 ImagesCat. No.: HY-111360RCAS No.: 2195361-33-0SPL-707 (Standard) is the analytical standard of SPL-707 (HY-111360). This product is intended for research and analytical applications. SPL-707 is an orally active, selective signal peptide peptidase-like 2a (SPPL2a) inhibitor with an IC50 of 77 nM for hSPPL2a. SPL-707 inhibits γ-secretase (IC50=6.1 μM) and SPP (IC50=3.7 μM). SPL-707 has the potential for autoimmune diseases research by targeting B cells and dendritic cells.
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Fosciclopirox (Standard)
0 ImagesCat. No.: HY-109174RCAS No.: 1380539-06-9Synonyms: CPX-POM (Standard)Fosciclopirox (Standard) is the analytical standard of Fosciclopirox (HY-109174). This product is intended for research and analytical applications. Fosciclopirox (CPX-POM) suppresses growth of urothelial cancer by targeting the γ-secretase complex. Fosciclopirox selectively delivers the active metabolite, Ciclopirox (CPX), to the entire urinary tract. Ciclopirox has anticancer activity in a number of solid and hematologic malignancies.
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BI-1408
0 ImagesCat. No.: HY-112282CAS No.: 2231075-94-6BI-1408 is a potent γ secretase modulator with an IC50 of 0.04 μM for Aβ42.
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LY-411575 (isomer 3)
0 ImagesLY-411575 isomer 3 is an isomer of LY411575, which is a potent γ-secretase inhibitor.
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ELN318463 racemate
0 ImagesCat. No.: HY-50882ACAS No.: 851599-82-1ELN318463 racemate is the racemate of ELN318463. ELN318463 is an amyloid precursor protein (APP) selective γ-secretase inhibitor. ELN318463 shows differential inhibition of presenilin (PS1)- and PS2-comprised γ-secretase with EC50s of 12nM and 656 nM for PS1and PS2, respectively. ELN318463 is 51-fold more selective for PS1.
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Itanapraced (Standard)
0 ImagesSynonyms: CHF5074 (Standard); CSP-1103 (Standard)Itanapraced (Standard) is the analytical standard of Itanapraced. This product is intended for research and analytical applications. Itanapraced (CHF5074) is an orally active γ-secretase modulator and a non-steroidal anti-inflammatory derivative. Itanapraced reduces Aβ42 and Aβ40 secretion with IC50 values of 3.6 and 18.4 μM, respectively. Itanapraced inhibits cell apoptosis of hippocampal neurons induced by oxygen and glucose deprivation (OGD). Itanapraced can be used for the research of Alzheimer's disease.
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DAPT (Standard)
0 ImagesCat. No.: HY-13027RCAS No.: 208255-80-5Synonyms: GSI-IX (Standard)DAPT (Standard) is the analytical standard of DAPT (HY-13027). This product is intended for research and analytical applications. DAPT (GSI-IX) is a potent and orally active γ-secretase inhibitor with IC50s of 115 nM and 200 nM for total amyloid-β (Aβ) and Aβ42, respectively. DAPT inhibits the activation of Notch 1 signaling and induces cell differentiation. DAPT also induces autophagy and apoptosis. DAPT has neuroprotection activity and has the potential for autoimmune and lymphoproliferative diseases, degenerative disease and cancers treatment.
