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 (82)
Antibodies (5)

By Effects:	Controls (2) Inhibitors (48) Modulators (27)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

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-16632

ELND 006	Inhibitor	99.7%
ELND 006 (Compound 30) is a metabolically stable γ-secretase inhibitor designed to selectively inhibit amyloid beta (Aβ) generation while sparing Notch signaling. It was developed through a synthetic strategy emphasizing diversity and chirality. ELND 006, along with its analog ELND007 (Compound 34), progressed into human clinical trials. In preclinical studies, both compounds demonstrated effective reduction of Aβ levels in vitro and in vivo. Comparisons with other γ-secretase inhibitors like Semagacestat, Begacestat, and Avagacestat underscored their potency and specificity in lowering Aβ levels in cerebrospinal fluid (CSF) of healthy human volunteers, suggesting potential therapeutic efficacy in Alzheimer's disease.

HY-14175

Begacestat		99.29%
Begacestat (GSI-953) is a selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase (IC₅₀Aβ₄₀=15 nM) for the treatment of Alzheimer's disease.

HY-171347

gamma-secretase modulator 6	Modulator
gamma-secretase modulator 6 (Example 50) is a gamma-secretase modulator. gamma-secretase modulator 6 inhibits Aβ42 secretion in HEK cell line stably expressing APP (Aβ amyloid precursor protein) (pIC₅₀: 8.1). gamma-secretase modulator 6 can be used for research of Alzheimer's disease.

HY-50754

gamma-secretase modulator 2	Modulator	98.80%
gamma-secretase modulator 2 is a potent and selective γ-secretase modulator for study of Alzheimer's disease.

HY-14176A

(1R,3S)-Compound E	Control	99.82%
(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.

HY-10043A

gamma-secretase modulator 1 hydrochloride	Modulator	99.85%
gamma-secretase inhibitior-1 is a gamma-secretase modulator, γ-secretase inhibitior-1 is useful for Alzheimer's disease.

HY-50889

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

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-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-145372

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

HY-148306

γ-Secretase modulator 14	Modulator
γ-Secretase modulator 14 is a γ-secretase modulator. γ-Secretase modulator 14 has the potenial for Alzheimer's disease (AD) research (WO2013010904A1; compound 42).

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-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
γ-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.

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.

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γ-secretase

γ-secretase

γ-secretase Related Products (82)

Antibodies (5)

γ-secretase Related Products (82):