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APP Inhibitor

" in MedChemExpress (MCE) Product Catalog:

58

Inhibitors & Agonists

2

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7

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1

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-128090A
    Apstatin TFA

    		Aminopeptidase Cardiovascular Disease
    Apstatin TFA is a potent aminopeptidase P (APP) inhibitor with Ki values of 2.6, 0.64 µM for rat and human APP, respectively. Apstatin TFA shows cardioprotection .
    Apstatin TFA
  • HY-136499
    DI-82

    		DNA/RNA Synthesis Cancer
    DI-82 is a potent deoxycytidine kinase (dCK) inhibitor with an IC50 app of 27.8 nM and Ki app of 9.2 nM. DI-82 has antitumor activity .
    DI-82
  • HY-50759
    Ispinesib
    5+ Cited Publications

    SB-715992

    		 Kinesin Apoptosis Cancer
    Ispinesib is a specific inhibitor of kinesin spindle protein (KSP), with a Ki app of 1.7 nM.
    Ispinesib
  • HY-12856
    GSK503
    5+ Cited Publications

    		 Histone Methyltransferase Cancer
    GSK503 is a potent and specific inhibitor of EZH2 methyltransferase with Ki app values of 3 to 27 nM.
    GSK503
  • HY-114174
    Fmoc-Ala-Glu-Asn-Lys-NH2
    2 Publications Verification

    		 Amyloid-β Neurological Disease
    Fmoc-Ala-Glu-Asn-Lys-NH2 is a selective asparagine endopeptidase (AEP) inhibitor peptide and suppresses amyloid precursor protein (APP) cleavage. AEP, a pH-controlled cysteine proteinase, is activated during ageing and mediates APP proteolytic processing .
    Fmoc-Ala-Glu-Asn-Lys-NH2
  • HY-108643
    CMPD1

    		MAPKAPK2 (MK2) Cancer
    CMPD1 is a selective and non-ATP-competitive p38 MAPK-mediated MK2 phosphorylation inhibitor with apparent Ki (Ki app) of 330 nM .
    CMPD1
  • HY-128090
    Apstatin

    		Aminopeptidase Cardiovascular Disease
    Apstatin is a potent aminopeptidase P (APP) inhibitor with Ki values of 2.6, 0.64 µM for rat and human APP, respectively. Apstatin shows cardioprotection .
    Apstatin
  • HY-147672
    IleRS-IN-1

    		Aminoacyl-tRNA Synthetase Infection
    IleRS-IN-1 (compound 11) is a potent and selective isoleucyl-tRNA synthetase (IleRS) inhibitor, with a Ki,app of 88 nM .
    IleRS-IN-1
  • HY-147674
    Isoleucyl tRNA synthetase-IN-2

    		Aminoacyl-tRNA Synthetase Infection
    Isoleucyl tRNA synthetase-IN-2 (compound 36a) is a potent and selective isoleucyl-tRNA synthetase (IleRS) inhibitor, with a Ki,app of 114 nM .
    Isoleucyl tRNA synthetase-IN-2
  • HY-128464
    LL320

    		Others Metabolic Disease
    LL320 is a selective NNMT inhibitor with a Ki,app of 6.8 nM. LL320 exhibits interactions with RNMT, DPH5, and SAHH .
    LL320
  • HY-15294
    CZC24832

    		PI3K Inflammation/Immunology Cancer
    CZC24832 is a highly selective and potent PI3Kγ inhibitor (IC50=27 nM) with apparent dissociation constants (Kd app) of 19 nM.
    CZC24832
  • 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).
    BMS 299897
  • HY-12989
    LDN-91946

    		Deubiquitinase Neurological Disease Cancer
    LDN-91946 is a potent, selective and uncompetitive ubiquitin C-terminal hydrolase-L1 (UCH-L1) inhibitor with a Ki app of 2.8 μM .
    LDN-91946
  • HY-16009B
    Buntanetap L-Tartrate

    (+)-Phenserine L-Tartrate; ANVS401 L-Tartrate

    		 Amyloid-β Cancer
    Buntanetap (L-Tartrate) is an orally administered small molecule inhibitor of several neurotoxic proteins. Buntanetap reduces amyloid precursor protein (APP) production by blocking its mRNA translation .
    Buntanetap L-Tartrate
  • HY-149397
    FXIIa-IN-2

    		Thrombin Cardiovascular Disease
    FXIIa-IN-1-IN-2 (Compound 21) is a Factor XIIa inhibitor (Ki app: 62.2 nM). FXIIa-IN-1-IN-2 can be used for research of thrombosis .
    FXIIa-IN-2
  • HY-149396
    FXIIa-IN-1

    		Thrombin Cardiovascular Disease
    XIIa-IN-1-IN-3 (Compound 22) is a Factor XIIa inhibitor (Ki app: 97.8 nM). XIIa-IN-1-IN-3 can be used for research of thrombosis .
    FXIIa-IN-1
  • HY-106005
    MMV390048
    3 Publications Verification

    		 Parasite PI4K Infection
    MMV390048 is a representative of a new chemical class of Plasmodium PI4K inhibitor (Kd app=0.3 µM). MMV390048 binds to the ATP binding site of Plasmodium PI4K and does not bind to other P. falciparum and human kinases apart from human PIP4K2C, thus alleviating potential kinase-mediated safety concerns. MMV390048 is an antimalarial agent .
    MMV390048
  • HY-128585
    GNE684

    		RIP kinase Inflammation/Immunology Cancer
    GNE684 is a potent inhibitor of potent receptor interacting protein 1 (RIP1), with mean Ki app values of 21 nM, 189 nM and 691 nM for human mouse and rat RIP1, respectively .
    GNE684
  • HY-144739
    BACE1-IN-8

    		Beta-secretase Neurological Disease
    BACE1-IN-8 (compound 70b) is a potent BACE1 (β-site APP cleaving enzyme 1) inhibitor, with an IC50 of 3.9 µM .
    BACE1-IN-8
  • HY-144741
    BACE1-IN-9

    		Beta-secretase Neurological Disease
    BACE1-IN-9 (compound 82b) is a potent BACE1 (β-site APP cleaving enzyme 1) inhibitor, with an IC50 of 1.2 µM .
    BACE1-IN-9
  • HY-107164
    Thiomarinol A

    4-Hydroxythiomarinol C

    		 Antibiotic Bacterial Infection
    Thiomarinol A (4-Hydroxythiomarinol C) is a potent antibiotic. Thiomarinol A is a hybrid of dithiolopyrrolone and marinolic acid. Thiomarinol A shows antimicrobial activity. Thiomarinol A inhibits MRSA IleRS in a dose-dependent with a Ki app value of 19 nM .
    Thiomarinol A
  • HY-153986
    AEP-IN-2

    		Cathepsin Neurological Disease
    AEP-IN-2 is an asparagine endopeptidase (AEP) inhibitor via block AEP cleavage of APP and Tau. AEP-IN-2 has oral activity and decreases Aβ40 and Aβ42 and p-Tau levels .
    AEP-IN-2
  • HY-105940
    IQB-782

    		Amino Acid Derivatives Cardiovascular Disease
    IQB-782 is a cysteine derivative. IQB-782 has inhibition for thrombin activatable fibrinolysis inhibitor (TAFI), with an Ki(app) of 0.14 μM. IQB-782 shows a potent mucolytic-expectorant activity .
    IQB-782
  • HY-135618
    DHODH-IN-3

    		Dihydroorotate Dehydrogenase DNA/RNA Synthesis Infection
    DHODH-IN-3 (compound 3) is a potent inhibitor of Human Dihydroorotate Dehydrogenases (HsDHODH) with an IC50 value of 261 nM. DHODH-IN-3 binds to the the ubiquinone binding cavities in DHODH with a Ki app of 32 nM. DHODH-IN-3 has the potential for malaria treatment .
    DHODH-IN-3
  • HY-108966
    Kushenol C

    		Beta-secretase Inflammation/Immunology
    Kushenol C, isolated from the roots of Sophora flavescens, shows anti-Inflammatory and anti-oxidative stress activities. Kushenol C inhibits BACE1 (β-site APP cleaving enzyme 1) with an IC50 of 5.45 µM .
    Kushenol C
  • HY-16009
    Buntanetap

    (+)-Phenserine; ANVS401

    		 α-synuclein Neurological Disease Inflammation/Immunology
    Buntanetap ((+)-Phenserine) is a multiple neurotoxic protein translation inhibitor with oral activity, including amyloid precursor protein (APP), α-synuclein (αSYN) and huntingtin protein (HTT). Buntanetap has anti-inflammatory effects and can be used in the study of Alzheimer's disease and Parkinson's disease .
    Buntanetap
  • HY-124322
    NB-360

    		Beta-secretase Neurological Disease Inflammation/Immunology
    NB-360 is a potent, brain penetrable, and orally bioavailable dual BACE1/BACE2 inhibitor (IC50: mouse and human BACE1=5 nM; BACE2=6 nM). NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in amyloid precursor protein(APP) transgenic mice. NB-360 can completely block the progression of Aβ deposition in the brains of APP transgenic mice. NB-360 shows excellent selectivity over the related aspartyl proteases pepsin, cathepsin D and cathepsin E .
    NB-360
  • 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 .
    III-31-C
  • HY-103374
    Phenserine

    (-)-Eseroline phenylcarbamate; (-)-Phenserine

    		 Cholinesterase (ChE) Amyloid-β Neurological Disease
    Phenserine ((-)-Eseroline phenylcarbamate) is a derivative of Physostigmine and is a potent, noncompetitive, long-acting and selective AChE inhibitor. Phenserine reduces β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ) formation. Phenserine improves cognitive performance and attenuates the progression of Alzheimer's disease .
    Phenserine
  • HY-103374A
    Phenserine tartrate

    (-)-Eseroline phenylcarbamate tartrate; (-)-Phenserine (+)-tartrate

    		 Cholinesterase (ChE) Amyloid-β Neurological Disease
    Phenserine tartrate ((-)-Eseroline phenylcarbamate) is a derivative of Physostigmine and is a potent, noncompetitive, long-acting and selective AChE inhibitor. Phenserine tartrate reduces β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ) formation. Phenserine tartrate improves cognitive performance and attenuates the progression of Alzheimer's disease .
    Phenserine tartrate
  • HY-N0192
    Arbutin
    1 Publications Verification

    β-Arbutin

    		 Tyrosinase Endogenous Metabolite Cancer
    Arbutin (β-Arbutin) is a competitive inhibitor of tyrosinase, with Ki app values of 1.42 mM for monophenolase; 0.9 mM for diphenolase. Arbutin is also used as depigmenting agents . Arbutin is a natural polyphenol isolated from the bearberry plant Arctostaphylos uvaursi, possesses with anti-oxidant, anti-inflammatory and anti-tumor properties .
    Arbutin
  • HY-N12249
    7-Deoxy-trans-dihydronarciclasine

    		Amyloid-β TMV Infection Neurological Disease Inflammation/Immunology
    7-Deoxy-trans-dihydronarciclasine, an alkaloid, is a tobacco mosaic virus (TMV) inhibitor (IC50: 1.80 μM). 7-Deoxy-trans-dihydronarciclasine is an anti-neuroinflammatory agent. 7-Deoxy-trans-dihydronarciclasine decreases the Aβ and APP levels in the cerebral cortex of Tg2576 mice .
    7-Deoxy-trans-dihydronarciclasine
  • HY-136733
    Ac-DNLD-CHO

    Ac-Asp-Asn-Leu-Asp-CHO

    		 Caspase Infection Neurological Disease
    Ac-DNLD-CHO (Ac-Asp-Asn-Leu-Asp-CHO) is a Caspase-3/7 inhibitor (IC50: 9.89, 245 nM respectively; Ki app: 0.68, 55.7 nM respectively). Ac-DNLD-CHO can be used for research of caspase-mediated apoptosis diseases, such as neurodegenerative disorders and viral infection diseases .
    Ac-DNLD-CHO
  • HY-129133
    cis-Miyabenol C

    		Drug Isomer Others
    cis-Miyabenol C is an isomer of the resveratrol trimer Miyabenol C, which can be isolated from grape herbs. Miyabenol C is an inhibitor of β-amyloid (Aβ) and amyloid β precursor protein (APP) in Alzheimer's disease model mice, and inhibit β-secretase activity without changing the protein level of β-secretase BACE1 .
    cis-Miyabenol C
  • HY-18010
    PCI 29732
    3 Publications Verification

    		 Btk BCRP Inflammation/Immunology
    PCI 29732 is a potent, orally active, reversible BTK inhibitor with Ki app values of 8.2, 4.6, and 2.5 nM for BTK, Lck and Lyn, respectively. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase. PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2 .
    PCI 29732
  • HY-168859
    JNK3 inhibitor-9

    		JNK GSK-3 Amyloid-β Neurological Disease
    JNK3 inhibitor-9 (Compound 24a) is a potent, selective and BBB-permeable JNK3 inhibitor with an IC50 value of 12 nM. JNK3 inhibitor-9 also potently inhibits GSK3α/β (IC50s: 14 and 35 nM, respectively) involved in Tau phosphorylation. JNK3 inhibitor-9 reduces c-Jun and APP phosphorylation. JNK3 inhibitor-9 protects neurons from Aβ1-42 toxicity .
    JNK3 inhibitor-9
  • HY-10254
    Mirdametinib
    Maximum Cited Publications
    111 Publications Verification

    PD0325901; PD325901

    		 MEK Autophagy Apoptosis Cancer
    Mirdametinib (PD0325901) is an orally active, selective and non-ATP-competitive MEK inhibitor with an IC50 of 0.33 nM. Mirdametinib exhibits a Ki app of 1 nM against activated MEK1 and MEK2. Mirdametinib suppresses the expression of p-ERK1/2 and induces apoptosis. Mirdametinib has anti-cancer activity for a broad spectrum of human tumor xenografts .
    Mirdametinib
  • HY-171347
    gamma-secretase modulator 6

    		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-N1414A
    3′,6-Disinapoylsucrose

    		Bcl-2 Family Apoptosis Neurological Disease
    3′,6-Disinapoylsucrose is a type of oligosaccharide that's effective when taken orally, and it has antidepressant, anti-anxiety, and antioxidant properties. 3′,6-Disinapoylsucrose inhibits neuronal apoptosis by lowering the ratio of Bax to Bcl-2 in hippocampal neurons, and it enhances cognitive function in APP/PS1 transgenic mice by activating the CREB/BDNF signaling pathway .
    3′,6-Disinapoylsucrose
  • HY-126047B
    (R)-(+)-Anatabine

    		NF-κB Amyloid-β nAChR Neurological Disease Inflammation/Immunology
    (R)-(+)-Anatabine is an less active R-enantiomer of Anatabine. Anatabine is a potent α4β2 nAChR agonist . Anatabine inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment .
    (R)-(+)-Anatabine
  • 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 .
    ELN318463
  • HY-19918A
    Anatabine dicitrate

    		NF-κB Amyloid-β nAChR Neurological Disease Inflammation/Immunology
    Anatabine dicitrate is a tobacco alkaloid that can cross the blood-brain barrier. Anatabine dicitrate is a potent α4β2 nAChR agonist. Anatabine dicitrate inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine dicitrate has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment .
    Anatabine dicitrate
  • 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 .
    ELN318463 racemate
  • HY-120597
    SAK3

    		Calcium Channel Neurological Disease
    SAK3 is a potent T-type voltage-gated Ca 2+ channels (T-VGCCs) enhancer. SAK3 enhances Cav3.1 and Cav3.3 T-type Ca 2+ channel currents. Acute SAK3 administration improves memory deficits in olfactory-bulbectomized mice . SAK3 inhibits amyloid β plaque formation in APP-KI mice by activating the proteasome activity .
    SAK3
  • HY-145286
    IMPDH2-IN-2

    		Bacterial Infection Cancer
    IMPDH2-IN-2 is a potent inhibitor of inosine 5’-monophosphate dehydrogenase (IMPDH) with a Ki,app value of 14 μM, respectively. IMPDH2-IN-2 displays moderate antibacterial activity (MIC = 6.3 and 11 μM in minimal GAST/Fe and rich 7H9/ADC/Tween media, respectively). IMPDH2-IN-2 is a potential anti-tuberculosis agent .
    IMPDH2-IN-2
  • HY-124832
    δ-Secretase inhibitor 11
    1 Publications Verification

    		 Caspase Amyloid-β Neurological Disease
    δ-Secretase inhibitor 11 (compound 11) is an orally active, potent, BBB-penetrated, non-toxic, selective and specific δ-secretase inhibitor, with an IC50 of 0.7 μM. δ-Secretase inhibitor 11 interacts with both the active site and allosteric site of δ-secretase. δ-Secretase inhibitor 11 attenuates tau and APP (amyloid precursor protein) cleavage. δ-Secretase inhibitor 11 ameliorates synaptic dysfunction and cognitive impairments in tau P301S and 5XFAD transgenic mouse models. δ-Secretase inhibitor 11 can be used for Alzheimer's disease research .
    δ-Secretase inhibitor 11
  • HY-13438
    AZD3839 free base
    1 Publications Verification

    		 Beta-secretase Neurological Disease
    AZD3839 is an orally available, selective, reversible inhibitor of the β-site amyloid precursor protein cleaving enzyme BACE1 that can cross the blood-brain barrier. AZD3839 inhibits recombinant human BACE1 with a Ki=26.1 nM. AZD3839 inhibits A40 production in SH-SY5Y cells with an IC50 of 4.8 nM. AZD3839 binds to BACE1 and reduces the Aβ amyloid produced by the cleavage of amyloid precursor protein (APP) by BACE1 and γ-secretase. AZD3839 can be used in the field of Alzheimer's disease research .
    AZD3839 free base
  • HY-19369
    L-685458
    5 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 .
    L-685458
  • HY-103490
    Takinib
    20+ Cited Publications

    EDHS-206

    		 MAP3K Apoptosis Infection Inflammation/Immunology Cancer
    Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM) .
    Takinib
  • HY-168241
    Flucopride

    		Cholinesterase (ChE) 5-HT Receptor Infection
    Flucopride (Compound 4a) is an AChE inhibitor (IC50: 24 nM), and a partial 5-HT4R agonist (Ki: 9.6 nM for (h)5-HT4R). Flucopride promotes the non-amyloidogenic processing of APP in COS-7 transiently expressing (h)5-HT4R (EC50: 23.0 nM). Flucopride may has good gastrointestinal track (GIT) penetration, and blood-brain barrier (BBB) cross-membrane penetration (PAMPA assay) .
    Flucopride

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