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-108714

NGP555	Modulator	98.77%
NGP555 is a γ-secretase modulator. NGP555 Lowers the Amyloid Biomarker Aβ42.

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-117482

BPN-15606	Modulator	99.96%
BPN-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.

HY-109174

Fosciclopirox	Inhibitor	99.66%
Fosciclopirox 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.

HY-111360

SPL-707	Inhibitor	99.94%
SPL-707 is an orally active, selective signal peptide peptidase-like 2a (SPPL2a) inhibitor with an IC₅₀ of 77 nM for hSPPL2a. SPL-707 inhibits γ-secretase (IC₅₀=6.1 μM) and SPP (IC₅₀=3.7 μM). SPL-707 has the potential for autoimmune diseases research by targeting B cells and dendritic cells.

HY-15185B

Nirogacestat dihydrobromide	Inhibitor	99.63%
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-50883

BMS 299897	Inhibitor	99.64%
BMS 299897 is a sulfonamide γ-secretase inhibitor with an IC₅₀ of 7 nM for Aβ production inhibition in HEK293 cells stably overexpressing amyloid precursor protein (APP).

HY-145343

RO7185876	Modulator	99.04%
RO7185876 is a potent and selective gamma secretase modulator as a potential research for Alzheimer's disease.

HY-B1786A

(E/Z)-Sulindac sulfide	Modulator	99.88%
(E/Z)-Sulindac sulfide is a potent γ-secretase modulator (GSM). (E/Z)-Sulindac sulfide selectively reduces Aβ42 production in favor of shorter Aβ species. (E/Z)-Sulindac sulfide can be used for researching Alzheimer’s disease.

HY-100604

JNJ-40418677	Modulator	≥99.0%
JNJ-40418677 is an orally active modulator of γ-secretase, can cross the blood-brain barrier. JNJ-40418677 inhibits Aβ42 and NS2B-NS3 protease, with IC₅₀s of 200 nM and 3.9 μM, respectively. JNJ-40418677 displays good biological tolerance, can be use for Alzheimer’s disease research.

HY-115726

FRM-024	Modulator	99.45%
FRM-024 is a potent CNS-penetrant gamma secretase modulator for familial Alzheimer’s disease.

HY-119165

GSM-1	Modulator	98.39%
GSM-1 is a potent γ-secretase modulator. GSM-1 directly targets the transmembrane domain (TMD) 1 of presenilin 1 (PS1).

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-10043

gamma-secretase modulator 1	Modulator	≥98.0%
γ-secretase inhibitior-1 is a gamma-secretase modulator, γ-secretase inhibitior-1 is useful for 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 treatment of Alzheimer's disease IC50 value: Target: γ-secretase γ-secretase modulator is modulation of the action of γ-secretase so as to Selectively attenuate production of Aβ(1-42) and hence find use in treatment or prevention of diseases associated with deposition of Aβ in the brain.

HY-136866

Aβ42-IN-2	Inhibitor	98.00%
Aβ42-IN-2 is a γ-secretase modulator extracted from patent WO2016070107, compound example 36. 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.

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-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-50882

ELN318463	Inhibitor	99.45%
ELN318463 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.

HY-12465

Z-Ile-Leu-aldehyde	Inhibitor
Z-Ile-Leu-aldehyde (Z-IL-CHO) is a potent and competitive peptide aldehyde inhibitor of γ-secretase and notch.

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γ-secretase

γ-secretase

γ-secretase Related Products (77)

Antibodies (5)

γ-secretase Related Products (77):