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 (104)
Antibodies (5)

By Effects:	Inhibitors (63) Controls (3) Modulators (32)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-13027

DAPT	Inhibitor	99.97%
DAPT (GSI-IX) is a potent and orally active γ-secretase inhibitor with IC₅₀s of 115 nM and 200 nM for total amyloid-β (Aβ) and Aβ₄₂, respectively. DAPT inhibits the activation of Notch 1 signaling and induces cell differentiation. DAPT also induces autophagy and apoptosis. DAPT has neuroprotection activity and has the potential for autoimmune and lymphoproliferative diseases, degenerative disease and cancers treatment.

HY-14176

Compound E	Inhibitor	99.97%
Compound E is a γ-secretase inhibitor. Compound E blocks β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage with IC₅₀s of 0.24, 0.37, 0.32 nM, respectively.

HY-50752

LY-411575	Inhibitor	98.68%
LY-411575 is a potent γ-secretase inhibitor with IC₅₀ of 0.078 nM/0.082 nM (membrane/cell-based), and also inhibits Notch S3 cleavage with an IC₅₀ of 0.39 nM.

HY-15185

Nirogacestat	Inhibitor	99.83%
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.

HY-13526

YO-01027	Inhibitor	99.59%
YO-01027 (Dibenzazepine;DBZ) is a potent γ-secretase inhibitor with IC₅₀ values of 2.92 and 2.64 nM for Notch and APPL cleavage, respectively.

HY-123761

L505-yne	Inhibitor
L505-yne is an active site-directed γ-secretase inhibitor. L505-yne blocks photoaffinity labeling of PS1-NTF, PS1-CTF, and SPP by clickable GSI photoprobes, binds the γ-secretase complex and inhibits Aβ42 production. L458-BPyne can be used for the research of Alzheimer’s disease.

HY-117521

EVP-0015962	Inhibitor
EVP-0015962 is an orally active, blood-brain barrier-permeable γ-secretase inhibitor with an IC₅₀ of 3.9 μM. EVP-0015962 alters γ-secretase-mediated cleavage of amyloid precursor protein, reduces Aβ₄₂ production and increases Aβ₃₈ production. EVP-0015962 reduces Aβ aggregates, amyloid plaques and inflammatory markers in the brains of mice, and improves their cognitive impairment. EVP-0015962 can be used for the research of Alzheimer's disease.

HY-128391

AZ1136	Modulator
AZ1136 is a highly selective γ-secretase modulator (GSM). AZ1136 reduces the levels of Aβ42 and Aβ40, with its IC₅₀ being 990 and 1400 nM. AZ1136 increases the levels of Aβ39 and Aβ37, but does not affect Aβ38. AZ1136 can be used for the study of Alzheimer's disease.

HY-11102

RO4929097	Inhibitor	99.01%
RO4929097 is an orally active γ secretase inhibitor with an IC₅₀ of 4 nM, inhibiting cellular processing of Aβ40 and Notch with EC₅₀ of 14 nM and 5 nM, respectively.

HY-10974

MK-0752	Inhibitor	99.02%
MK-0752 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 crosses the blood-brain barrier. MK-0752 reduces newly generated CNS Aβ in vivo.

HY-12449

Crenigacestat	Inhibitor	99.01%
Crenigacestat (LY3039478) is an orally active Notch and γ-secretase inhibitor, with an IC₅₀ of 1 nM in most of the tumor cell lines tested.

HY-19369

L-685458	Inhibitor	99.69%
L-685458 is a potent transition state analog (TSA) γ-secretase inhibitor (GSI). L-685458 inhibits amyloid β-protein precursor γ-secretase activity with IC₅₀ of 17 nM, shows greater than 50-100-fold selectivity over other aspartyl proteases tested. L685458 inhibits γ-secretase-mediated cleavage of APP-C99 and Notch-100 with IC₅₀s of 301.3 nM and 351.3 nM, respectively. L-685458 can be used for the research of alzheimer’s disease (AD) and cancers.

HY-10009

Semagacestat	Inhibitor	98.61%
Semagacestat is a γ-secretase inhibitor, inhibits β-amyloid (Aβ42), Aβ38 and Aβ40 with IC₅₀s of 10.9, 12 and 12.1 nM, respectively; also inhibits Notch signaling with IC₅₀ of 14.1 nM. Semagacestat can be used for the research of alzheimer's disease.

HY-15185B

Nirogacestat dihydrobromide	Inhibitor	99.81%
Nirogacestat dihydrobromide (PF-3084014 dihydrobromide) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC₅₀ of 6.2 nM. Inhibition of Notch signaling by Nirogacestat dihydrobromide while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers.

HY-50845

Avagacestat	Inhibitor	99.92%
Avagacestat (BMS-708163) is a potent inhibitor of γ-secretase, with IC₅₀s of 0.27 nM and 0.30 nM for Aβ42 and Aβ40 inhibition; Avagacestat (BMS-708163) also inhibits NICD (Notch IntraCellular Domain) with IC₅₀ of 0.84 nM and shows weak inhibition of CYP2C19, with IC₅₀ of 20 μM. Avagacestat can be used for Alzheimer disease research.

HY-14399

Itanapraced	Inhibitor	99.37%
Itanapraced (CHF5074) is an orally active γ-secretase modulator and a non-steroidal anti-inflammatory derivative. Itanapraced reduces Aβ42 and Aβ40 secretion with IC₅₀ values of 3.6 and 18.4 μM, respectively. Itanapraced inhibits cell apoptosis of hippocampal neurons induced by oxygen and glucose deprivation (OGD). Itanapraced can be used for the research of Alzheimer's disease.

HY-10016

E 2012	Modulator
E 2012 is a potent gamma (γ) secretase modulator without affecting Notch processing. E 2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis. E 2012 aims at Alzheimer's disease by reduction of amyloid β-42, and induces cataract following repeated doses in the rat.

HY-14174

MRK-560	Inhibitor	99.0%
MRK-560, a chemical probe, is an orally active, brain barrier-penetrated γ-Secretase inhibitor, reducing Aβ peptide in rat brain and cerebrospinal fluid. MRK-560 decreases mutant NOTCH1 processing by selectively inhibiting PSEN1. MRK-560 can be used in studies of Alzheimer's disease and T-cell acute lymphoblastic leukaemia (T-ALL).

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.

HY-15670

BMS-906024	Inhibitor	99.91%
BMS-906024 is an orally active and selective γ-secretase (gamma secretase) inhibitor. BMS-906024 is a potent pan-Notch receptors inhibitor with IC₅₀s of 1.6 nM, 0.7 nM, 3.4 nM, and 2.9 nM for Notch1, -2, -3, and -4 receptors, respectively. BMS-906024 demonstrates broad-spectrum antineoplastic activity.

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γ-secretase

γ-secretase

γ-secretase Related Products (104)

Antibodies (5)

γ-secretase Related Products (104):