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    Stem Cell/Wnt
  4. γ-secretase

γ-secretase

Gamma secretase

γ-secretase

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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).

γ-secretase Produits associés (65):

Cat. No. Nom du produit Effet Pureté Chemical Structure
  • HY-13027G
    DAPT (GMP)
    		Inhibitor
    DAPT (GSI-IX) (GMP) is DAPT (HY-13027) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. DAPT is a potent and orally active γ-secretase inhibitor.
    DAPT (GMP)
  • HY-130609
    Aβ42-IN-1
    		Inhibitor
    Aβ42-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.
    Aβ42-IN-1
  • HY-130609A
    Aβ42-IN-1 free base
    		Modulator
    Aβ42-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.
    Aβ42-IN-1 free base
  • HY-112282
    BI-1408
    		Modulator
    BI-1408 is a potent γ secretase modulator with an IC50 of 0.04 μM for Aβ42.
    BI-1408
  • HY-13526G
    YO-01027 (GMP)
    		Inhibitor
    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.
    YO-01027 (GMP)
  • HY-103539
    3,5-Bis(4-nitrophenoxy)benzoic acid
    		Inhibitor
    3,5-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.
    3,5-Bis(4-nitrophenoxy)benzoic acid
  • HY-103537
    (Rac)-BIIB042
    		Modulator
    (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.
    (Rac)-BIIB042
  • HY-115726
    FRM-024
    		Modulator
    FRM-024 is a potent CNS-penetrant gamma secretase modulator for familial Alzheimer’s disease.
    FRM-024
  • HY-145372
    γ-Secretase modulator 10
    		Modulator
    γ-Secretase modulator 10 is a novel γ-secretase modulator.
    γ-Secretase modulator 10
  • HY-145428
    BT-GSI
    		Inhibitor
    BT-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.
    BT-GSI
  • HY-108499
    NNC 26-9100
    		Inhibitor
    NNC 26-9100 is a selective somatostatin sst4 receptor full agonist (Ki: 6 nM, EC50: 2 nM). NNC 26-9100 decreases total soluble Aβ42, increases brain neprilysin activity and improves learning.
    NNC 26-9100
  • HY-120234
    Z-LLNle-CHO
    		Inhibitor
    Z-LLNle-CHO (Z-Leu-Leu-Nle-CHO) is a γ-secretase inhibitor I. Z-LLNle-CHO induces caspase and ROS-dependent apoptosis by blocking the Akt-mediated pro-survival pathway. Z-LLNle-CHO can be used in cancer research, such as breast cancer and leukaemia.
    Z-LLNle-CHO
  • HY-156012
    PSEN1-IN-2
    		Inhibitor
    PSEN1-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.
    PSEN1-IN-2
  • HY-147720
    γ-Secretase modulator 11
    5-{8-[(3,4'- difluoro [1,1'- biphenyl]-4-yl) methoxy] - 2-methylimidazo [1,2-a] pyridin-3-yl}-n-methylpyridin-2-formamide (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.
    γ-Secretase modulator 11
  • HY-117482A
    BPN-15606 besylate
    		Modulator
    BPN-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.
    BPN-15606 besylate
  • HY-156011
    PSEN1-IN-1
    		Inhibitor
    PSEN1-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.
    PSEN1-IN-1
  • HY-B1786S
    Sulindac sulfide-d3
    		Inhibitor
    Sulindac 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.
    Sulindac sulfide-d<sub>3</sub>
  • HY-50884
    BMS 433796
    		Inhibitor
    BMS 433796 is a γ-secretase inhibitor with Aβ lowering activity in a transgenic mouse model of Alzheimer's disease.
    BMS 433796
  • HY-P4295
    Z-Phe-Ala-diazomethylketone
    		Inhibitor
    Z-Phe-Ala-diazomethylketone binds directly to Aβ42 monomers and small oligomers. Z-Phe-Ala-diazomethylketone inhibits the formation of Aβ42 dodecamers and inhibits Aβ42 fibril formation in the solution. Z-Phe-Ala-diazomethylketone has the potential for neurodegenerative disorders research.
    Z-Phe-Ala-diazomethylketone
  • HY-146151
    γ-Secretase modulator 12
    		Modulator
    γ-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.
    γ-Secretase modulator 12