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Gamma secretase

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Beta-secretase (1) GABA Receptor (1) γ-secretase (73) Amyloid-β (16) Apoptosis (10) Autophagy (1) Cholinesterase (ChE) (1) Drug Metabolite (2) Notch (13) Organoid (2) Phosphodiesterase (PDE) (1) Proteasome (2)
By Research Areas:	Cancer (24) Inflammation/Immunology (5) Metabolic Disease (5) Neurological Disease (65)

Inhibitors & Agonists

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Fluorescent Dye

Biochemical Assay Reagents

Peptides

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Products

Recombinant Proteins

Isotope-Labeled Compounds

Targets Recommended: γ-secretase Beta-secretase Legumain GABA Receptor CD74

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-10043

gamma-secretase modulator 1	γ-secretase	Neurological Disease
γ-secretase inhibitior-1 is a gamma-secretase modulator, γ-secretase inhibitior-1 is useful for Alzheimer's disease.

HY-10043A

gamma-secretase modulator 1 hydrochloride	γ-secretase	Neurological Disease
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	γ-secretase	Neurological Disease
gamma-secretase modulator 3 is a gamma-secretase modulator.

HY-50754

gamma-secretase modulator 2	γ-secretase	Neurological Disease
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-50900

gamma-Secretase Modulators Amyloid-β production inhibitor; γ-secretase Modulators	Amyloid-β	Neurological Disease
gamma-Secretase Modulators (Amyloid-β production inhibitor) is a Amyloid-β production inhibitor.

HY-150050

gamma-secretase modulator 5	Amyloid-β	Neurological Disease
gamma-secretase modulator 5 (compound 22d) is a brain-penetrant gamma-secretase modulator (GSMs) that inhibits the production of the aggregated amyloid β-peptide Aβ42 with an IC₅₀ value of 60 nM. gamma-secretase modulator 5 can be used in the study of Alzheimer's disease .

HY-117381

*γ-secretase-IN-2*	γ-secretase	Neurological Disease
γ-secretase-IN-2 (Compound 36) is an inhibitor for *γ-secretase, with an IC₅₀* of 0.07 nM .

HY-145372

*γ-Secretase* modulator 10**	γ-secretase	Neurological Disease
γ-Secretase modulator 10 is a novel *γ-secretase* modulator.

HY-148306

*γ-Secretase* modulator 14**	γ-secretase	Neurological Disease
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-147720A

*γ-Secretase* modulator 11 hydrochloride**	γ-secretase	Neurological Disease
γ-Secretase modulator 11 hydrochloride (compound 1o) is a potent and orally active *γ-secretase* modulator with an IC₅₀ of 0.029 µM. γ-Secretase modulator 11 hydrochloride induces a robust reduction in brain Aβ42 levels. γ-Secretase modulator 11 hydrochloride rescues cognitive deficits exhibited by AD model mice. γ-Secretase modulator 11 hydrochloride has the potential for the research of alzheimer's disease .

HY-150049

*γ-Secretase* modulator 13**	Amyloid-β	Neurological Disease
γ-Secretase modulator 13 (compound 4) is a gamma-secretase modulator (GSMs) that inhibits the production of the aggregated amyloid β-peptide Aβ42 with an IC₅₀ value of 163 nM. γ-Secretase modulator 13 can be used in the study of Alzheimer's disease .

HY-146151

*γ-Secretase* modulator 12**	γ-secretase Amyloid-β	Neurological Disease
γ-Secretase modulator 12 (Compound 1a) is a *γ-secretase* modulator that can selectively decrease amyloid-β42 (Aβ42) levels (IC₅₀ of 0.39 µM). γ-Secretase modulator 12 can be used for Alzheimer’s disease research. γ-Secretase modulator 12 has a good brain/plasma ratio (Kp, brain = 0.72) in mice .

HY-111205

*γ-Secretase* modulator 16**	Others	Others
γ-Secretase modulator 16 is an active compound.

HY-128581

*γ-Secretase* modulator 4**	γ-secretase	Neurological Disease
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-14176

Compound E 5+ Cited Publications γ-secretase-IN-1	γ-secretase	Cancer
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-12465

Z-Ile-Leu-aldehyde 2 Publications Verification Z-IL-CHO; GSI-XII; γ-secretase inhibitor XII	Notch γ-secretase Apoptosis	Cancer
Z-Ile-Leu-aldehyde (Z-IL-CHO) is a potent and competitive peptide aldehyde inhibitor of *γ-secretase* and notch .

HY-B1786

Sulindac sulfide 1 Publications Verification cis-Sulindac sulfide	Drug Metabolite γ-secretase	Neurological Disease
Sulindac sulfide is a noncompetitive *γ-secretase* inhibitor, with an IC₅₀ of 20.2 μM for γ₄₂-secretase activity.

HY-B1786S

Sulindac sulfide-d3 cis-Sulindac sulfide-d₃	γ-secretase	Neurological Disease
Sulindac sulfide-d₃ is deuterium labeled Sulindac sulfide. Sulindac sulfide is a noncompetitive γ-secretase inhibitor, with an IC50 of 20.2 μM for γ42-secretase activity.

HY-B1786R

Sulindac sulfide (Standard)	Drug Metabolite γ-secretase	Neurological Disease
Sulindac sulfide (Standard) is the analytical standard of Sulindac sulfide. This product is intended for research and analytical applications. Sulindac sulfide is a noncompetitive γ-secretase inhibitor, with an IC50 of 20.2 μM for γ42-secretase activity.

HY-159836

Nivegacetor	γ-secretase	Neurological Disease
Nivegacetor is a potent *γ-secretase* modulator .

HY-N2319

Dihydroergocristine mesylate DHEC mesylate	Amyloid-β	Neurological Disease
Dihydroergocristine mesylate (DHEC mesylate) is a inhibitor of γ-secretase (GSI), reduces the production of the Alzheimer's disease amyloid-β peptides, binds directly to γ-secretase and Nicastrin with equilibrium dissociation constants (K_d) of 25.7 nM and 9.8 μM, respectively .

HY-145343

RO7185876	γ-secretase	Neurological Disease
RO7185876 is a potent and selective **gamma secretase** modulator as a potential research for Alzheimer's disease.

HY-147720

*γ-Secretase* modulator 11**	γ-secretase	Neurological Disease
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-115726

FRM-024	γ-secretase	Neurological Disease
FRM-024 is a potent CNS-penetrant **gamma secretase** modulator for familial Alzheimer’s disease.

HY-N2319R

Dihydroergocristine mesylate (Standard) DHEC mesylate (Standard)	Amyloid-β	Neurological Disease
Dihydroergocristine (mesylate) (Standard) is the analytical standard of Dihydroergocristine (mesylate). This product is intended for research and analytical applications. Dihydroergocristine mesylate (DHEC mesylate) is a inhibitor of γ-secretase (GSI), reduces the production of the Alzheimer's disease amyloid-β peptides, binds directly to γ-secretase and Nicastrin with equilibrium dissociation constants (K_d) of 25.7 nM and 9.8 μM, respectively .

HY-50752A

LY-411575 isomer 1	γ-secretase	Neurological Disease
LY-411575 isomer 1 is an isomer of LY411575, which is a potent γ-secretase inhibitor.

HY-50884

BMS 433796	γ-secretase	Neurological Disease
BMS 433796 is a *γ-secretase* inhibitor with Aβ lowering activity in a transgenic mouse model of Alzheimer's disease.

HY-50752B

LY-411575 (isomer 2)	γ-secretase	Neurological Disease
LY-411575 isomer 2 is an isomer of LY411575, which is a potent γ-secretase inhibitor.

HY-50752C

LY-411575 (isomer 3)	γ-secretase	Neurological Disease
LY-411575 isomer 3 is an isomer of LY411575, which is a potent γ-secretase inhibitor.

HY-108714

NGP555	γ-secretase	Neurological Disease
NGP555 is a *γ-secretase* modulator. NGP555 Lowers the Amyloid Biomarker Aβ42 .

HY-112282

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

HY-19369

L-685458 4 Publications Verification L-685,458	γ-secretase Apoptosis	Neurological Disease Cancer
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-50882

ELN318463	γ-secretase	Neurological Disease
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-15670

BMS-906024 2 Publications Verification	γ-secretase Notch	Cancer
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 .

HY-50882A

ELN318463 racemate	γ-secretase	Neurological Disease
ELN318463 racemate is the racemate of ELN318463. 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 12nM and 656 nM for PS1and PS2, respectively. ELN318463 is 51-fold more selective for PS1 .

HY-14176A

(1R,3S)-Compound E	Others	Cancer
(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-13526

YO-01027 4 Publications Verification Dibenzazepine; DBZ	Notch γ-secretase	Cancer
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-115726A

(-)-FRM-024	γ-secretase	Neurological Disease
(-)-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-12449

Crenigacestat 4 Publications Verification LY3039478	Notch γ-secretase	Cancer
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-50883

BMS 299897	γ-secretase	Neurological Disease
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-11102

RO4929097 10+ Cited Publications RG-4733	γ-secretase Notch	Neurological Disease Cancer
RO4929097 (RG-4733) is a γ secretase inhibitor with IC₅₀ of 4 nM, inhibiting cellular processing of Aβ40 and Notch with EC₅₀ of 14 nM and 5 nM, respectively .

HY-19550

PF-06442609	γ-secretase	Neurological Disease
PF-06442609 is an orally active *γ‑secretase* modulator, with an IC₅₀ of 6 nM for Aβ42. PF-06442609 possesses brain good penetration .

HY-119165

GSM-1	γ-secretase	Neurological Disease
GSM-1 is a potent *γ-secretase* modulator. GSM-1 directly targets the transmembrane domain (TMD) 1 of presenilin 1 (PS1) .

HY-164451

GSI-18	γ-secretase Notch	Cancer
GSI-18 is a γ-secretase inhibitor with anticancer activity. GSI-18 attenuates anchorage-independent growth in pancreatic cancer cells by inhibiting Notch signaling .

HY-14175

Begacestat GSI-953	γ-secretase	Neurological Disease
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-50752

LY-411575 10+ Cited Publications	Organoid γ-secretase Notch Apoptosis	Neurological Disease
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 IC₅₀ of 0.39 nM.

HY-109174

Fosciclopirox CPX-POM	γ-secretase	Metabolic Disease Cancer
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-103538

JLK-6	Amyloid-β	Neurological Disease
JLK-6 markedly reduce the production of amyloid β-peptide (Aβ) by amyloid-β Precursor protein (APP) expressing HEK293 cells by affecting the γ-secretase cleavage of APP, with no effect on the cleavage of the Notch receptor .

HY-13027G

DAPT GSI-IX	γ-secretase	Neurological Disease Inflammation/Immunology Cancer
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-15211

MRK 003	γ-secretase Apoptosis	Neurological Disease Cancer
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 .

Cat. No.	Product Name

HY-L013

Neuronal Signaling Compound Library

2,710 compounds

Neuronal Signaling is involved in the regulation of the mechanisms of the central nervous system (CNS) such as its structure, function, genetics and physiology as well as how this can be applied to understand diseases of the nervous system. Every information processing system in the CNS is composed of neurons and glia, neurons have evolved unique capabilities for intracellular signaling (communication within the cell) and intercellular signaling (communication between cells). G protein-coupled receptors (GPCRs), including 5-HT receptor, histamine receptor, opioid receptor, etc. are the largest class of sensory proteins and are important therapeutic targets in Neuronal Signaling. Besides, Notch signaling, such as β- and γ-secretase, also plays multiple roles in the development of the CNS including regulating neural stem cell (NSC) proliferation, survival, self-renewal and differentiation. GPCR dysfunction caused by receptor mutations and environmental challenges contributes to many neurological diseases. Notch signaling in neurons, glia, and NSCs is also involved in pathological changes that occur in disorders such as stroke, Alzheimer's disease and CNS tumors. Thus, targeting Neuronal Signaling, such as notch signaling and GPCRs, can be used as therapeutic interventions for several different CNS disorders.

MCE designs a unique collection of 2,710 Neuronal Signaling-related compounds that act as a useful tool for the research of neuronal regulation and neuronal diseases.

HY-L017

Stem Cell Signaling Compound Library

1,846 compounds

Adult stem cells are important for tissue homeostasis and regeneration due to their ability to self-renew and generate multiple types of differentiated daughters. Self-renewal is reflected by their capacity to undergo multiple/limitless divisions. Several signaling pathways are involved in self-renewal of stem cells, that is, Notch, Wnt, and Hedgehog pathways or Polycomb family proteins. Recent studies mainly focus on cancer stem cell (CSCs), induced pluripotent stem cell (iPSCs), neural stem cell and maintenance of embryonic stem cell pluripotency. Among them, CSCs have been believed to be responsible for tumor initiation, growth, and recurrence that have implications for cancer therapy.

MCE owns a unique collection of 1,846 compounds that can be used for stem cell regulatory and signaling pathway research.

Cat. No.	Product Name	Type

HY-13027G

DAPT (GMP) GSI-IX (GMP)	Fluorescent Dye
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-13526G

YO-01027 (GMP) Dibenzazepine (GMP); DBZ (GMP)	Fluorescent Dye
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 .

Cat. No.	Product Name	Type

HY-13027G

DAPT (GMP) GSI-IX (GMP)	Biochemical Assay Reagents
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-13526G

YO-01027 (GMP) Dibenzazepine (GMP); DBZ (GMP)	Biochemical Assay Reagents
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 .

Cat. No.	Product Name	Target	Research Area

HY-120234

Z-LLNle-CHO Z-Leu-Leu-Nle-CHO; GSII	γ-secretase Proteasome Apoptosis	Cancer
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-P3779

Amyloid 17-42 Aβ(17-42)	Apoptosis	Neurological Disease
Amyloid 17-42 (Aβ(17-42)) is a major constituent of diffuse plaques in Alzheimer's disease and cerebellar pre-amyloid in Down's syndrome, derived by alpha- and gamma-secretase cleavage of the amyloid precursor protein (APP). Amyloid 17-42 can induce neuronal apoptosis via a Fas-like/caspase-8 activation pathway .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N1280

Semilicoisoflavone B	Structural Classification Flavonoids Leguminosae Source classification Phenols Polyphenols Plants Glycyrrhiza uralensis Fisch. Isoflavones	Amyloid-β
Semilicoisoflavone B, an isoflavone, mainly derived from Glycyrrhiza uralensis Fisch.. Semilicoisoflavone B reduces amyloid β (Aβ) secretion by inhibiting β-secretase-1 (BACE1) expression and activity. Semilicoisoflavone B decreases BACE1 expression mainly through increasing PPARγ expression and inhibiting STAT3 phosphorylation .

Cat. No.	Compare	Product Name	Species	Source

HY-P702211

	APH1A Protein, Human (Cell-Free, His, SUMO) Gamma-secretase subunit APH-1A; Aph-1alpha; Presenilin-stabilization factor	Human	E. coli Cell-free
	The APH1A protein is a noncatalytic subunit of the γ-secretase complex and is essential for the assembly of this endoprotease. The γ-secretase complex, including presenilin homodimer, nicastrin, APH1A, and PSENEN/PEN2, catalyzes the cleavage of intramembrane proteins such as Notch and APP. APH1A Protein, Human (Cell-Free, His, SUMO) is the recombinant human-derived APH1A protein, expressed by E. coli Cell-free , with N-6*His, N-SUMO labeled tag. The total length of APH1A Protein, Human (Cell-Free, His, SUMO) is 247 a.a., with molecular weight of 42.9 kDa.

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HY-B1786S

Sulindac sulfide-d3
Sulindac sulfide-d₃ is deuterium labeled Sulindac sulfide. Sulindac sulfide is a noncompetitive γ-secretase inhibitor, with an IC50 of 20.2 μM for γ42-secretase activity.

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Gamma secretase

Inhibitors & Agonists

Screening Libraries

Fluorescent Dye

Biochemical Assay Reagents

Peptides

NaturalProducts

Recombinant Proteins

Isotope-Labeled Compounds

Natural
Products