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 (83)
Antibodies (5)

By Effects:	Controls (2) Inhibitors (49) Modulators (27)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

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-18614

LY900009	Inhibitor	99.79%
LY900009 is a potent and orally active, First-in-class inhibitor of Notch signaling via selective inhibition of the γ-secretase protein (GSI). LY900009 inhibits Notch signalling in tumor cell lines and endothelial cells (IC₅₀=0.005-20 nM). LY900009 can be used for advanced cancer research.

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-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-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-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-108714

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

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-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-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-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-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-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-115726A

(-)-FRM-024	Modulator	98.27%
(-)-FRM-024 is the (-)-isomer of FRM-024, a potent CNS-penetrant gamma secretase modulator that can be utilized in Alzheimer’s disease research.

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-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.

HY-100604A

(R)-JNJ-40418677	Control	99.27%
(R)-JNJ-40418677 is the R-enantiomer of JNJ-40418677 (HY-100604).

HY-136866

Aβ42-IN-2	Inhibitor	98.00%
Aβ42-IN-2 (compound example 36) is a γ-secretase modulator. 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.

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γ-secretase

γ-secretase

γ-secretase Related Products (83)

Antibodies (5)

γ-secretase Related Products (83):