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Results for "

gamma+secretase+inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Amyloid-β (10) Apoptosis (9) Autophagy (1) Biochemical Assay Reagents (1) Drug Metabolite (2) Isotope-Labeled Compounds (1) Notch (12) Organoid (2) Proteasome (1) Reference Standards (3) γ-secretase (44)
By Research Areas:	Cancer (22) Inflammation/Immunology (2) Metabolic Disease (2) Neurological Disease (29)

Inhibitors & Agonists

Fluorescent Dyes

Biochemical Assay Reagents

Peptides

Isotope-Labeled Compounds

GMP Molecules

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13027

DAPT Maximum Cited Publications 158 Publications Verification GSI-IX	Organoid γ-secretase Amyloid-β Autophagy Notch Apoptosis	Neurological Disease Inflammation/Immunology Cancer
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-13526

YO-01027 5+ Cited Publications 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-50752

LY-411575 25+ 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 an IC₅₀ of 0.39 nM.

HY-14176

Compound E 15+ Cited Publications γ-Secretase-IN-1	γ-secretase	Cancer
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-11102

RO4929097 15+ Cited Publications	γ-secretase Notch	Neurological Disease Cancer
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-15185

Nirogacestat 10+ Cited Publications PF-3084014	γ-secretase Apoptosis	Neurological Disease Cancer
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-10974

MK-0752 10+ Cited Publications	γ-secretase	Neurological Disease Cancer
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 5+ Cited Publications 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-10009

Semagacestat 10+ Cited Publications LY450139	γ-secretase Amyloid-β Notch	Neurological Disease
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-19369

L-685458 5+ Cited Publications 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-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-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-15185B

Nirogacestat dihydrobromide 10+ Cited Publications PF-3084014 dihydrobromide; PF-03084014 dihydrobromide	γ-secretase Apoptosis	Cancer
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-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-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-15670

BMS-906024 3 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-14174

MRK-560 4 Publications Verification	γ-secretase	Neurological Disease Cancer
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-76562

Methyl 6-bromopicolinate	Biochemical Assay Reagents	Others
Methyl 6-bromopicolinate is a synthetic intermediate used in the preparation of *γ-secretase* inhibitor library scaffolds .

HY-16632

ELND 006	γ-secretase Amyloid-β	Metabolic Disease
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-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-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 .

HY-158012

LY3056480	γ-secretase	Others
LY3056480 is a gamma-secretase inhibitor (GSI) that inhibits Notch signaling. LY3056480 improves mild to moderate sensorineural hearing loss and is safe and tolerable. Intratympanic administration of LY3056480 induces hair cell regeneration and partial hearing recovery in mammals .

HY-171348

Amyloid-β-IN-2	Amyloid-β γ-secretase	Neurological Disease
Amyloid-β-IN-2 (Compound EX.112) is a selective *γ-secretase* inhibitor. Amyloid-β-IN-2 inhibits Aβ42 secretion in H4 cells with an EC₅₀ value of 226 nM. Amyloid-β-IN-2 is promising for research of Alzheimer's disease (AD) and other diseases related to Aβ deposition .

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-13526G

YO-01027 Dibenzazepine; DBZ	Notch γ-secretase	Cancer
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-14176A

(1R,3S)-Compound E	γ-secretase	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-14176G

Compound E γ-Secretase-IN-1	γ-secretase	Cancer
Compound E (GMP) is a GMP-grade Compound E (HY-14176). GMP-grade small molecules can be used as adjuvant reagents in cell therapy. Compound E is a *γ-secretase* inhibitor. Compound E inhibits β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage with IC₅₀ values of 0.24, 0.37, and 0.32 nM, respectively .

HY-171349

Amyloid-β-IN-3	γ-secretase Amyloid-β	Neurological Disease
Amyloid-β-IN-3 (EX.113) is a selective *γ-secretase* inhibitor. Amyloid-β-IN-3 inhibits Aβ42 secretion in H4 cells with an EC₅₀ value of 148 nM. Amyloid-β-IN-3 regulates the γ-secretase catalytic activity to decrease Aβ42 production, thereby alleviating neurotoxicity caused by Aβ deposition. Amyloid-β-IN-3 is promising for research of Alzheimer's disease (AD) .

HY-164451

GSI-18	γ-secretase Notch	Cancer
GSI-18 is a γ-secretase inhibitor with anticancer activity. GSI-18 inhibits the attachment-free growth of pancreatic cancer cells by inhibiting Notch signaling .

HY-15185R

Nirogacestat (Standard) PF-3084014 (Standard)	γ-secretase Apoptosis Reference Standards	Cancer
Nirogacestat (Standard) is the analytical standard of Nirogacestat. This product is intended for research and analytical applications. 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-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-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-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-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-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-B1786S

Sulindac sulfide-d3 cis-Sulindac sulfide-d₃	Isotope-Labeled Compounds 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) cis-Sulindac sulfide (Standard)	Drug Metabolite Reference Standards 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-16633

ELND 007	γ-secretase Amyloid-β	Metabolic Disease
ELND 007 (Compound 34) is a metabolically stable γ-secretase inhibitor designed to selectively inhibit amyloid beta (Aβ) generation while minimizing Notch inhibition. Developed alongside ELND 006 (Compound 30), it underwent human clinical trials following a synthetic strategy emphasizing diversity and chirality. In preclinical studies, ELND 007 showed promising in vitro and in vivo characteristics, effectively reducing Aβ levels. Comparative studies with other γ-secretase inhibitors like Semagacestat, Begacestat, and Avagacestat highlighted its efficacy in lowering Aβ production, particularly demonstrated by reduced Aβ levels in the cerebrospinal fluid (CSF) of healthy human volunteers, suggesting potential therapeutic benefit for Alzheimer's disease .

HY-145428

BT-GSI	Notch γ-secretase	Cancer
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-139052

III-31-C	γ-secretase	Neurological Disease
III-31-C is a (hydroxyethyl)urea *γ-secretase* inhibitor. III-31-C inhibits Aऔ production with an IC₅₀ of 10 nM in the cell-free γ-secretase assay and 200 nM in APP-transfected cells. III-31-C can be used in Alzheimer's disease research .

HY-10975

MK-0752 sodium	γ-secretase	Neurological Disease Cancer
MK-0752 sodium 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 sodium crosses the blood-brain barrier. MK-0752 sodium reduces newly generated CNS Aβ in vivo .

HY-145343A

(9R)-RO7185876	γ-secretase Amyloid-β	Neurological Disease
(9R)-RO7185876 (Compound example 16) is a *γ-secretase* inhibitor. (9R)-RO7185876 inhibits Αβ42 secretion. (9R)-RO7185876 can be used for the researches of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, multi-infarct dementia, dementia pugilistica or Down syndrome .

HY-10009R

Semagacestat (Standard) LY450139 (Standard)	Reference Standards γ-secretase Amyloid-β Notch	Neurological Disease
Semagacestat (Standard) is the analytical standard of Semagacestat. This product is intended for research and analytical applications. 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-123761

L505-yne	γ-secretase	Neurological Disease
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-18157

SCH 900229	Amyloid-β	Neurological Disease
SCH 900229 is a potent γ-secretase inhibitor with selective activity against PS1. The Aβ40 IC50 value of SCH 900229 is 1.3 nM, showing its excellent ability in reducing Aβ. SCH 900229 has shown good Aβ-lowering effects after oral administration in preclinical animal models. SCH 900229 has been advanced to human clinical trials for further development of compounds for the inhibition of Alzheimer's disease .

HY-117521

EVP-0015962	γ-secretase Amyloid-β	Neurological Disease
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 .

Cat. No.	Product Name	Type

HY-13027G

DAPT GSI-IX	Fluorescent Dyes
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 Dibenzazepine; DBZ	Fluorescent Dyes
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-14176G

Compound E γ-Secretase-IN-1	Fluorescent Dyes
Compound E (GMP) is a GMP-grade Compound E (HY-14176). GMP-grade small molecules can be used as adjuvant reagents in cell therapy. Compound E is a *γ-secretase* inhibitor. Compound E inhibits β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage with IC₅₀ values of 0.24, 0.37, and 0.32 nM, respectively .

Cat. No.	Product Name	Type

HY-13027G

DAPT GSI-IX	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-76562

Methyl 6-bromopicolinate	Biochemical Assay Reagents
Methyl 6-bromopicolinate is a synthetic intermediate used in the preparation of *γ-secretase* inhibitor library scaffolds .

HY-13526G

YO-01027 Dibenzazepine; DBZ	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 .

HY-14176G

Compound E γ-Secretase-IN-1	Biochemical Assay Reagents
Compound E (GMP) is a GMP-grade Compound E (HY-14176). GMP-grade small molecules can be used as adjuvant reagents in cell therapy. Compound E is a *γ-secretase* inhibitor. Compound E inhibits β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage with IC₅₀ values of 0.24, 0.37, and 0.32 nM, respectively .

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 .

Cat. No.	Product Name	Chemical Structure

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.

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-13526G

YO-01027 Dibenzazepine; DBZ	Notch γ-secretase	Cancer
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-14176G

Compound E γ-Secretase-IN-1	γ-secretase	Cancer
Compound E (GMP) is a GMP-grade Compound E (HY-14176). GMP-grade small molecules can be used as adjuvant reagents in cell therapy. Compound E is a *γ-secretase* inhibitor. Compound E inhibits β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage with IC₅₀ values of 0.24, 0.37, and 0.32 nM, respectively .

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