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Results for "

γ-Secretase

" in MedChemExpress (MCE) Product Catalog:

114

Inhibitors & Agonists

2

Screening Libraries

3

Fluorescent Dyes

4

Biochemical Assay Reagents

2

Peptides

1

Inhibitory Antibodies

2

Natural
Products

1

Recombinant Proteins

1

Isotope-Labeled Compounds

1

Oligonucleotides

3

GMP Molecules

Targets Recommended:
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 42, 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 .
    DAPT
  • 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.
    Compound E
  • 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.
    YO-01027
  • 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.
    LY-411575
  • HY-15185
    Nirogacestat
    10+ Cited Publications

    PF-3084014

    γ-secretase Apoptosis 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 .
    Nirogacestat
  • 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 .
    MK-0752
  • HY-18236
    MDL-28170
    15+ Cited Publications

    Calpain Inhibitor III

    Proteasome Neurological Disease Inflammation/Immunology
    MDL-28170 (Calpain Inhibitor III) is a potent, selective and membrane-permeable cysteine protease inhibitor of calpain that rapidly penetrates the blood-brain barrier following systemic administration . MDL-28170 also block γ-secretase .
    MDL-28170
  • HY-50845
    Avagacestat
    2 Publications Verification

    BMS-708163

    γ-secretase Notch Cancer
    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.
    Avagacestat
  • 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 .
    Crenigacestat
  • 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 .
    Semagacestat
  • 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 .
    L-685458
  • HY-171306

    Liposome Others
    MK16 is a lipid material that can be used to construct blood-brain barrier penetrable lipid nanoparticles for mRNA delivery. MK16 facilitates blood-brain barrier crossing via γ-secretase-mediated and caveolae-mediated transcytosis. MK16 can be used for drug delivery research .
    MK16
  • 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 .
    Z-Ile-Leu-aldehyde
  • HY-14399
    Itanapraced
    1 Publications Verification

    CHF5074; CSP-1103

    γ-secretase Apoptosis Neurological Disease
    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 .
    Itanapraced
  • 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 .
    Nirogacestat dihydrobromide
  • HY-159836

    RG6289

    γ-secretase Neurological Disease
    Nivegacetor is a potent γ-secretase modulator .
    Nivegacetor
  • HY-13027G

    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 .
    DAPT
  • HY-120789

    γ-secretase Neurological Disease
    PF-06648671 is a novel, brain-penetrable, and orally active γ-secretase modulator (GSM). PF-06648671 reduces Aβ42 and Aβ40, with concomitant increases in Aβ37 and Aβ38 in vitro. PF-06648671 is used for the study of Alzheimer’s disease .
    PF-06648671
  • 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.
    Sulindac sulfide
  • HY-50883

    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).
    BMS 299897
  • 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 .
    BMS-906024
  • 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) .
    MRK-560
  • HY-100604

    γ-secretase Amyloid-β Neurological Disease
    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 .
    JNJ-40418677
  • HY-76562

    Biochemical Assay Reagents Others
    Methyl 6-bromopicolinate is a synthetic intermediate used in the preparation of γ-secretase inhibitor library scaffolds .
    Methyl 6-bromopicolinate
  • HY-N2319
    Dihydroergocristine mesylate
    1 Publications Verification

    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 (Kd) of 25.7 nM and 9.8 μM, respectively .
    Dihydroergocristine mesylate
  • HY-10043

    γ-secretase Neurological Disease
    γ-secretase inhibitior-1 is a gamma-secretase modulator, γ-secretase inhibitior-1 is useful for Alzheimer's disease.
    gamma-secretase modulator 1
  • HY-18614

    Notch γ-secretase Cancer
    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 .
    LY900009
  • HY-150049

    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 .
    γ-Secretase modulator 13
  • HY-108714

    γ-secretase Neurological Disease
    NGP555 is a γ-secretase modulator. NGP555 Lowers the Amyloid Biomarker Aβ42 .
    NGP555
  • HY-111360
    SPL-707
    1 Publications Verification

    γ-secretase Inflammation/Immunology
    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 .
    SPL-707
  • HY-119165

    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) .
    GSM-1
  • HY-117482

    γ-secretase Neurological Disease
    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 .
    BPN-15606
  • HY-171347

    γ-secretase Amyloid-β Neurological Disease
    gamma-secretase modulator 6 (Example 50) is a gamma-secretase modulator. gamma-secretase modulator 6 inhibits Aβ42 secretion in HEK cell line stably expressing APP (Aβ amyloid precursor protein) (pIC50: 8.1). gamma-secretase modulator 6 can be used for research of Alzheimer's disease .
    gamma-secretase modulator 6
  • HY-16632

    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 .
    ELND 006
  • HY-B1786A

    γ-secretase Amyloid-β Neurological Disease
    (E/Z)-Sulindac sulfide is a potent γ-secretase modulator (GSM). (E/Z)-Sulindac sulfide selectively reduces Aβ42 production in favor of shorter species. (E/Z)-Sulindac sulfide can be used for researching Alzheimer’s disease .
    (E/Z)-Sulindac sulfide
  • HY-120234

    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 .
    Z-LLNle-CHO
  • HY-145343

    γ-secretase Neurological Disease
    RO7185876 is a potent and selective gamma secretase modulator as a potential research for Alzheimer's disease.
    RO7185876
  • HY-171444

    γ-secretase Amyloid-β Neurological Disease
    GSM III is a γ-Secretase complexe (GSEC) modulator. GSM III significantly regulates amyloid-β (Aβ) length at the extracellular interface between the protease (NCT, PSEN) and the substrate APPC99. GSM III can be used for Alzheimer's disease (AD) research .
    GSM III
  • HY-171348

    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 .
    Amyloid-β-IN-2
  • HY-50882

    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 .
    ELN318463
  • HY-15211

    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 .
    MRK 003
  • HY-148306

    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) .
    γ-Secretase modulator 14
  • HY-14176G

    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 .
    Compound E
  • HY-146151

    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 .
    γ-Secretase modulator 12
  • HY-50900

    Amyloid-β production inhibitor; γ-Secretase Modulators

    Amyloid-β Neurological Disease
    gamma-Secretase Modulators (Amyloid-β production inhibitor) is a Amyloid-β production inhibitor.
    gamma-Secretase Modulators
  • HY-171349

    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) .
    Amyloid-β-IN-3
  • HY-145372

    γ-secretase Neurological Disease
    γ-Secretase modulator 10 is a novel γ-secretase modulator.
    γ-Secretase modulator 10
  • HY-147720A

    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 .
    γ-Secretase modulator 11 hydrochloride
  • HY-128581

    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 .
    γ-Secretase modulator 4
  • HY-14176A

    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.
    (1R,3S)-Compound E

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