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 (121)
Related Products (121)
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Antibodies (5)
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Aβ42-IN-1
0 ImagesCat. No.: HY-130609CAS No.: 2582757-69-3Aβ42-IN-1, compound 1v, is a novel, potent and orally active?γ-secretase modulator (GSM). Aβ42-IN-1 potently reduced Aβ42 levels with an IC50?value of 0.091?μM without CYP3A4 inhibition. Aβ42-IN-1 shows a sustained pharmacokinetic profile.
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LY3056480
0 ImagesCat. No.: HY-158012CAS No.: 2064292-78-8LY3056480 is a γ-secretase inhibitor. LY3056480 inhibits the Notch signaling pathway, upregulates Atoh1, promotes hair cell regeneration, and drives supporting cell transdifferentiation. LY3056480 is applicable to research related to sensorineural hearing loss.
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Aβ42-IN-1 free base
0 ImagesCat. No.: HY-130609ACAS No.: 2434633-17-5Aβ42-IN-1 free base (compound 1v) is an orally active, high brain exposure γ-secretase modulator. Aβ42-IN-1 free base potently reduces Aβ42 levels with an IC50 value of 0.091 μM, and significantly reduces brain Aβ42 levels in mice. Aβ42-IN-1 free base is a promising compound for the treatment of Alzheimer’s disease.
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L505-yne
0 ImagesCat. No.: HY-123761CAS No.: 1374647-07-0L505-yne is an active site-directed γ-secretase inhibitor. L505-yne blocks photoaffinity labeling of PS1-NTF, PS1-CTF, and SPP by clickable GSI photoprobes, binds the γ-secretase complex and inhibits Aβ42 production. L458-BPyne can be used for the research of Alzheimer’s disease.
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Fosciclopirox disodium
0 ImagesCat. No.: HY-109174ACAS No.: 1380539-08-1Synonyms: CPX-POM disodiumFosciclopirox disodium suppresses growth of urothelial cancer by targeting the γ-secretase complex. Fosciclopirox disodium selectively delivers the active metabolite, Ciclopirox (HY-B0450), to the entire urinary tract. Ciclopirox has anticancer activity in a number of solid and hematologic malignancies.
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YO-01027 (GMP)
0 ImagesCat. No.: HY-13526GCAS No.: 209984-56-5Synonyms: Dibenzazepine (GMP); DBZ (GMP)YO-01027 (Dibenzazepine) (GMP) is YO-01027 (HY-13526) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. YO-01027 is a potent γ-secretase inhibitor.
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3,5-Bis(4-nitrophenoxy)benzoic acid
0 Images3,5-Bis(4-nitrophenoxy)benzoic acid is an inhibitor of γ-secretase. 3,5-Bis(4-nitrophenoxy)benzoic acid causes a decrease in the released levels of Aβ42 and notch-1 Aβ-like peptide 25 (Nβ25). 3,5-Bis(4-nitrophenoxy)benzoic acid, as a marker for fetal hypothyroidism, is a 3,3’-diiodothyronine sulfate (T2S) cross-reactive material in maternal serum.
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(Rac)-BIIB042
0 ImagesCat. No.: HY-103537CAS No.: 1257395-14-4(Rac)-BIIB042 (Compound 10) is an modulator of γ-Secretase. (Rac)-BIIB042 reduces Amyloid-β 42 level with an EC50 value of 0.39 µM. (Rac)-BIIB042 can be used for the study of Alzheimer's disease.
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MK-0752 sodium
0 ImagesCat. No.: HY-10975CAS No.: 656810-87-6MK-0752 sodium 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 sodium crosses the blood-brain barrier. MK-0752 sodium reduces newly generated CNS Aβ in vivo.
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EVP-0015962
0 ImagesCat. No.: HY-117521CAS No.: 1447811-26-8EVP-0015962 is an orally active, blood-brain barrier-permeable γ-secretase inhibitor with an IC50 of 3.9 μM. EVP-0015962 alters γ-secretase-mediated cleavage of amyloid precursor protein, reduces Aβ42 production and increases Aβ38 production. EVP-0015962 reduces Aβ aggregates, amyloid plaques and inflammatory markers in the brains of mice, and improves their cognitive impairment. EVP-0015962 can be used for the research of Alzheimer's disease.
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(7RS)-Nivegacetor
0 ImagesCat. No.: HY-159836APurity: 98.87%Synonyms: (7RS)-RG6289(7RS)-Nivegacetor is the racemate of Nivegacetor (HY-159836). Nivegacetor is a potent and selective γ-secretase modulator. It reduces Aβ42 production and can be used in Alzheimer's disease research.
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JLK-6
0 ImagesCat. No.: HY-103538CAS No.: 62252-26-0JLK-6 is a rhomboid protease GlpG inhibitor. JLK-6 reduces the production of Amyloid β-peptide by altering the cleavage of β-amyloid precursor protein by γ-secretase, with no effect on the cleavage of Notch receptors. JLK-6 can be used in research related to Alzheimer's disease.
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γ-Secretase modulator 10
0 ImagesCat. No.: HY-145372CAS No.: 2694817-84-8γ-Secretase modulator 10 is a novel γ-secretase modulator.
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AZ1136
0 ImagesCat. No.: HY-128391CAS No.: 1380508-60-0AZ1136 is a γ-secretase modulator that regulates amyloid-β (Aβ) production without reducing total Aβ generation. AZ1136 also modulates γ-secretase-mediated Notch S4 cleavage, but does not inhibit NICD formation. AZ1136 can be used in studies related to γ-secretase, APP processing and Alzheimer's disease.
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γ-Secretase modulator 14
0 ImagesCat. No.: HY-148306CAS No.: 1420200-85-6γ-Secretase modulator 14 is a γ-secretase modulator. γ-Secretase modulator 14 has the potenial for Alzheimer's disease (AD) research (WO2013010904A1; compound 42).
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BT-GSI
0 ImagesCat. No.: HY-145428BT-GSI is a γ-secretase inhibitor (GSI) and a bone-targeted Notch inhibitor. BT-GSI has dual anti-myeloma and anti-resorptive properties, which can be used for the research of multiple myeloma and associated bone disease. BT-GSI inhibits tumor growth and osteolytic disease progression.
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BACE1-IN-1 hydrochloride
0 ImagesCat. No.: HY-100182ACAS No.: 1310349-35-9BACE1-IN-1 hydrochloride is an orally active, blood-brain barrier penetrant dual-target inhibitor of BACE1/2, with IC50 values of 23 nM and 24 nM against human BACE1 and BACE2, respectively. BACE1-IN-1 hydrochloride reduces cerebral Aβ40 levels in mice. BACE1-IN-1 hydrochloride can be used in studies related to Alzheimer's disease and type 2 diabetes.
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γ-Secretase modulator 11
0 ImagesCat. No.: HY-147720CAS No.: 2434630-29-0γ-Secretase modulator 11 (1o) showed high potency in vitro and brain exposure, inducing brain a β 42 levels were significantly reduced and showed undetectable inhibition of cytochrome P450 enzymes. In addition, compound 1o showed excellent anti cognitive deficit effect in AD model mice.
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BPN-15606 besylate
0 ImagesCat. No.: HY-117482ACAS No.: 2436239-00-6BPN-15606 besylate 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. BPN-15606 besylate lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 besylate has acceptable PK/PD properties, including bioavailability, half-life, and clearance.
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Anti-Nicastrin Antibody (A5226A)
0 ImagesCat. No.: HY-P992275Anti-Nicastrin Antibody (A5226A) is a monoclonal antibody against Nicastrin and an inhibitor of γ-secretase. Anti-Nicastrin Antibody (A5226A) recognizes the fully glycosylated mature presenilin enhancer in the active γ-secretase complex and inhibits its activity via competition for substrate binding. Anti-Nicastrin Antibody (A5226A) abrogates the growth of cancer cells dependent on γ-secretase activity. Anti-Nicastrin Antibody (A5226A) serves as an imaging tool to visualize the endocytic trafficking of active γ-secretase, and also acts as a detection reagent to evaluate the endocytic efficiency of γ-secretase. Anti-Nicastrin Antibody (A5226A) can be used in studies related to non-small cell lung cancer, T-cell acute lymphoblastic leukemia and Alzheimer's disease.
