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 (117)
Related Products (117)
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Antibodies (5)
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(R)-JNJ-40418677
0 Images(R)-JNJ-40418677 is the R-enantiomer of JNJ-40418677 (HY-100604).
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Theasaponin E1
0 ImagesTheasaponin E1 is an orally effective tea saponin. Theasaponin E1 inhibits the proliferation of cancer cells by activating apoptosis. Theasaponin E1 inhibits angiogenesis in ovarian cancer cells and HUVECs by reducing the expression of VEGF. Theasaponin E1 upregulates the phosphorylation level of ATM protein and the expression level of PTEN protein in cancer cells, decreases the phosphorylation levels of Akt, mTOR, p70S6K and 4E-BP1 proteins, downregulates the expression of HIF-1α and NF-κB, and reduces the protein expression of Notch ligands Dll4 and Jagged1. Theasaponin E1 exerts neuroprotective effects by inhibiting the activity of acetylcholinesterase, activating α-secretase and neprilysin, reducing the concentration of Aβ, and inhibiting the activities of β-secretase and γ-secretase. Theasaponin E1 exhibits toxic effects on cancer cells and quinone reductase-inducing activity, and inhibits tumor growth in vivo. Theasaponin E1 induces ferroptosis in Pomacea canaliculata by synergistically disrupting cholesterol homeostasis and sphingolipid metabolism. Theasaponin E1 possesses anti-biofilm activity against Candida albicans. Theasaponin E1 can be used in the research of ovarian cancer, obesity, Alzheimer's disease and fungal infections.
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(-)-FRM-024
0 Images(-)-FRM-024 is the (-)-isomer of FRM-024, a potent CNS-penetrant gamma secretase modulator that can be utilized in Alzheimer’s disease research.
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Z-Ile-Leu-aldehyde
0 ImagesCat. No.: HY-12465CAS No.: 161710-10-7Synonyms: Z-IL-CHO; GSI-XII; γ-Secretase inhibitor XIIZ-Ile-Leu-aldehyde (Z-IL-CHO) is a potent and competitive peptide aldehyde inhibitor of γ-secretase and notch.
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Z-LLNle-CHO
0 ImagesCat. No.: HY-120234CAS No.: 133407-83-7Synonyms: Z-Leu-Leu-Nle-CHO; GSII
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Nivegacetor
0 ImagesSynonyms: RG6289Nivegacetor (RG6289) a potent and selective γ-secretase modulator. Nivegacetor can reduce the production of Aβ42 can be used for the research of Alzheimer's disease.
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ELN318463
0 ImagesELN318463 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 12 nM and 656 nM for PS1 and PS2, respectively. ELN318463 is 51-fold more selective for PS1.
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Fosciclopirox
0 ImagesSynonyms: CPX-POMFosciclopirox (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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PSEN1-IN-2
0 ImagesPSEN1-IN-2 (Compound 13K) is a PSEN1 inhibitor. PSEN1-IN-2 inhibits PSEN1-APH1A and PSEN1-APH1B complex with IC50s of 6.9 and 2.4 nM. PSEN1-IN-2 can be used for Alzheimer's disease research.
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(9R)-RO7185876
0 Images(9R)-RO7185876 (Compound example 16) is a γ-secretase inhibitor. (9R)-RO7185876 inhibits Αβ42 secretion. (9R)-RO7185876 can be used for the researches of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, multi-infarct dementia, dementia pugilistica or Down syndrome.
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BPN-15606
0 ImagesBPN-15606 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 lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 has acceptable PK/PD properties, including bioavailability, half-life, and clearance.
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Nirogacestat (Standard)
0 ImagesSynonyms: PF-3084014 (Standard)Nirogacestat (Standard) is the analytical standard of Nirogacestat. This product is intended for research and analytical applications. Nirogacestat (PF-3084014) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC50 of 6.2 nM. Inhibition of Notch signaling by Nirogacestat while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers.
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L-Citronellol (Standard)
0 ImagesSynonyms: (S)-3,7-Dimethyloct-6-en-1-ol (Standard)L-Citronellol ((S)-3,7-Dimethyloct-6-en-1-ol) is an analytical standard for L-Citronellol (HY-W015515). This product is intended for research and analytical applications. L-Citronellol is a natural product with anti-allergic and neuroprotective effects. L-Citronellol inhibits mast cell activation and the release of inflammatory factors by inhibiting the ERK pathway. L-Citronellol inhibits BACE1/PSEN1 and AChE, reduces TNF-α expression and lipid peroxidation, demonstrating the potential of multi-target anti-Alzheimer's disease (AD).
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Aβ42-IN-2
0 ImagesAβ42-IN-2 (compound example 36) is a γ-secretase modulator. Aβ42-IN-2 has an IC50 of 6.5 nM for Αβ42. Aβ42-IN-2 can be used for the research of Alzheimer's disease.
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γ-Secretase modulator 4
0 Imagesγ-Secretase modulator 4 is a potent γ-secretase modulator, reduces the Aβ42 level with IC50s of 0.014 μM and 0.017 μM in human and mouse, respectively.
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gamma-secretase modulator 2
0 Imagesgamma-secretase modulator 2 is a potent and selective γ-secretase modulator for study of Alzheimer's disease.
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(1R,3S)-Compound E
0 Images(1R,3S)-Compound E is the isomer of Compound E (HY-14176), and can be used as an experimental control. Compound E is a γ-secretase inhibitor. Compound E bloks β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage with IC50s of 0.24, 0.37, 0.32 nM, respectively.
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gamma-secretase modulator 1 hydrochloride
0 Imagesgamma-secretase inhibitior-1 is a gamma-secretase modulator, γ-secretase inhibitior-1 is useful for Alzheimer's disease.
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gamma-secretase modulator 3
0 ImagesGamma-secretase modulator 3 is a γ-secretase modulator. Gamma-secretase modulator 3 has the potential for use in research on neurological diseases such as Alzheimer's disease.
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Demissidine
0 ImagesDemissidine is an alkaloid that can be isolated from potato. Demissidine is a promising dual inhibitors against β- and γ-secretase proteins in silico.
