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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MRK 003
0 ImagesCat. No.: HY-15211CAS No.: 623165-93-5MRK 003 is an orally active γ-secretase inhibitor. MRK 003 targets the Notch signaling pathway by blocking the proteolytic cleavage of Notch receptors. MRK 003 inhibits tumor cell proliferation, induces apoptosis, downregulates anti-apoptotic proteins, upregulates phosphorylated Akt, suppresses angiogenesis, and overcomes microenvironment-mediated proliferative protection. MRK 003 can be used in research related to lung cancer, multiple myeloma, non-Hodgkin's lymphoma, pancreatic ductal adenocarcinoma, glioblastoma, and breast cancer.
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BMS-932481
0 ImagesCat. No.: HY-117957CAS No.: 1263871-36-8BMS-932481 is an orally active modulator for γ-secretase, selectively reduce Aβ1-42 and Aβ1-40 production, with IC50s of 6.6 and 25.3 nM, respectively.
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Sulindac sulfide-d3
0 ImagesCat. No.: HY-B1786SCAS No.: 250608-66-3Synonyms: cis-Sulindac sulfide-d3Sulindac sulfide-d3 is deuterium labeled Sulindac sulfide. Sulindac sulfide is a noncompetitive γ-secretase inhibitor, with an IC50 of 20.2 μM for γ42-secretase activity.
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GSI-18
0 ImagesCat. No.: HY-164451CAS No.: 362653-62-1GSI-18 is a γ-secretase inhibitor with anticancer activity. GSI-18 inhibits the attachment-free growth of pancreatic cancer cells by inhibiting Notch signaling.
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ELND 007
0 ImagesCat. No.: HY-16633CAS No.: 1444006-79-4ELND 007 (Compound 34) is a metabolically stable γ-secretase inhibitor designed to selectively inhibit amyloid beta (Aβ) generation while minimizing Notch inhibition. Developed alongside ELND 006 (Compound 30), it underwent human clinical trials following a synthetic strategy emphasizing diversity and chirality. In preclinical studies, ELND 007 showed promising in vitro and in vivo characteristics, effectively reducing Aβ levels. Comparative studies with other γ-secretase inhibitors like Semagacestat, Begacestat, and Avagacestat highlighted its efficacy in lowering Aβ production, particularly demonstrated by reduced Aβ levels in the cerebrospinal fluid (CSF) of healthy human volunteers, suggesting potential therapeutic benefit for Alzheimer's disease.
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Compound E (GMP)
0 ImagesCat. No.: HY-14176GCAS No.: 209986-17-4Synonyms: γ-Secretase-IN-1 (GMP)Compound E (GMP) is a GMP-grade Compound E (HY-14176). GMP-grade small molecules can be used as adjuvant reagents in cell therapy. Compound E is a γ-secretase inhibitor. Compound E inhibits β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage with IC50 values of 0.24, 0.37, and 0.32 nM, respectively.
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BMS 433796
0 ImagesCat. No.: HY-50884CAS No.: 935525-13-6BMS 433796 is a γ-secretase inhibitor with Aβ lowering activity in a transgenic mouse model of Alzheimer's disease.
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γ-secretase-IN-2
0 ImagesCat. No.: HY-117381CAS No.: 564462-36-8γ-secretase-IN-2 (Compound 34) is an inhibitor for γ-secretase, with an IC50 of 0.06 nM. γ-secretase-IN-2 can be used for the study of Alzheimer's disease.
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BIIB042
0 ImagesCat. No.: HY-103537ACAS No.: 1257396-73-8BIIB042 is a potent, orally active, brain-penetrant, and selective γ-secretase modulator (GSM). BIIB042 reduces Aβ42 and increases Aβ38 levels in cells. BIIB042 significantly reduces brain Aβ42 levels in CF-1 mice and Fischer rats, as well as plasma Aβ42 levels in cynomolgus monkeys. BIIB042 reduces Aβ42 levels and Aβ plaque burden in Tg2576 mice. BIIB042 can be used for alzheimer's disease (AD) research.
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SSZ
0 ImagesSSZ is a multi-target inhibitor, which targets multiple pathological mechanisms of Alzheimer's disease (AD). SSZ targets acetylcholinesterase, butyrylcholinesterase, β-site amyloid precursor protein cleavage enzyme 1 (BACE1), and γ-secretase. SSZ ameliorates Alzheimer’s diseases and exhibits neuroprotective effect in mice.
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γ-Secretase modulator 12
0 ImagesCat. No.: HY-146151CAS No.: 2204249-82-9γ-Secretase modulator 12 (Compound 1a) is a γ-secretase modulator that can selectively decrease amyloid-β42 (Aβ42) levels (IC50 of 0.39 µM). γ-Secretase modulator 12 can be used for Alzheimer’s disease research. γ-Secretase modulator 12 has a good brain/plasma ratio (Kp, brain = 0.72) in mice.
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γ-Secretase modulator 11 hydrochloride
0 ImagesCat. No.: HY-147720ACAS No.: 2434630-30-3γ-Secretase modulator 11 hydrochloride (compound 1o) is a potent and orally active γ-secretase modulator with an IC50 of 0.029 µM. γ-Secretase modulator 11 hydrochloride induces a robust reduction in brain Aβ42 levels. γ-Secretase modulator 11 hydrochloride rescues cognitive deficits exhibited by AD model mice. γ-Secretase modulator 11 hydrochloride has the potential for the research of alzheimer's disease.
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III-31-C
0 ImagesCat. No.: HY-139052CAS No.: 398515-96-3III-31-C is a (hydroxyethyl)urea γ-secretase inhibitor. III-31-C inhibits Aऔ production with an IC50 of 10 nM in the cell-free γ-secretase assay and 200 nM in APP-transfected cells. III-31-C can be used in Alzheimer's disease research.
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BMS-869780
0 ImagesCat. No.: HY-18326CAS No.: 1235493-78-3BMS-869780 is an orally active non-acidic γ-secretase (γ-secretase) modulator. BMS-869780 regulates the activity of γ-secretase, thereby altering the production profile of β-amyloid proteins. When acting alone, it changes the relative levels of specific β-amyloid subtypes without inhibiting the total production of β-amyloid proteins. BMS-869780 exerts a synergistic effect with γ-secretase modulators of the acidic structural class to inhibit the total production of β-amyloid proteins in cell cultures.
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PF-06442609
0 ImagesCat. No.: HY-19550CAS No.: 1402002-76-9PF-06442609 is an orally active γ secretase modulator, with an IC50 of 6 nM for Aβ42. PF-06442609 possesses brain good penetration.
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Sulindac sulfide (Standard)
0 ImagesCat. No.: HY-B1786RCAS No.: 49627-27-2Synonyms: cis-Sulindac sulfide (Standard)Sulindac sulfide (Standard) is the analytical standard of Sulindac sulfide. This product is intended for research and analytical applications. Sulindac sulfide is a noncompetitive γ-secretase inhibitor, with an IC50 of 20.2 μM for γ42-secretase activity.
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Aminogenistein
0 ImagesCat. No.: HY-133184CAS No.: 132018-32-7Aminogenistein is a p56lck inhibitor with a 1.2 μM IC50. Aminogenistein inhibits production of Aβ1-40 and Aβ1-42 peptides. Aminogenistein induces accumulation of APP-CTFα and APP-CTFβ, indicating γ-secretase cleavage inhibition. Aminogenistein can be used for the research of alzheimer's disease.
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LY-411575 (Standard)
0 ImagesCat. No.: HY-50752RCAS No.: 209984-57-6
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LY-411575 (isomer 2)
0 ImagesLY-411575 isomer 2 is an isomer of LY411575, which is a potent γ-secretase inhibitor.
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(R)-JNJ-40418677 (Standard)
0 Images(R)-JNJ-40418677 (Standard) is the analytical standard of (R)-JNJ-40418677 (HY-100604A). This product is intended for research and analytical applications. (R)-JNJ-40418677 is the R-enantiomer of JNJ-40418677 (HY-100604).
