γ-secretase

Gamma secretase

γ-secretase

Related Products

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 Related Products (77)
Antibodies (5)

By Effects:	Inhibitors (46) Modulators (26)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-128581

γ-Secretase modulator 4	Modulator	99.47%
γ-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.

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.

HY-50889

gamma-secretase modulator 3	Modulator	≥98.0%
gamma-secretase modulator 3 is a gamma-secretase modulator.

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.

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.

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.

HY-109174A

Fosciclopirox disodium	Inhibitor
Fosciclopirox 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.

HY-112282

BI-1408	Modulator
BI-1408 is a potent γ secretase modulator with an IC₅₀ of 0.04 μM for Aβ₄₂.

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.

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.

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.

HY-10975

MK-0752 sodium	Inhibitor
MK-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.

HY-145372

γ-Secretase modulator 10	Modulator
γ-Secretase modulator 10 is a novel γ-secretase modulator.

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.

HY-108499

NNC 26-9100	Inhibitor
NNC 26-9100 is a selective somatostatin sst4 receptor full agonist (K_i: 6 nM, EC₅₀: 2 nM). NNC 26-9100 decreases total soluble Aβ42, increases brain neprilysin activity and improves learning.

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.

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.

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.

HY-15211

MRK 003	Inhibitor
MRK 003 is a potent, selective and orally active γ-secretase inhibitor. MRK 003 reduce brain Aβ production in vivo. MRK 003 induces caspase-dependent apoptosis and inhibits tumor cell proliferation in vivo and in vitro.

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.

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γ-secretase

γ-secretase

γ-secretase Related Products (77)

Antibodies (5)

γ-secretase Related Products (77):