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APP Inhibitor

" in MedChemExpress (MCE) Product Catalog:

83

Inhibitors & Agonists

3

Peptides

1

Inhibitory Antibodies

9

Natural
Products

1

Isotope-Labeled Compounds

2

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-10254
    Mirdametinib
    Maximum Cited Publications
    154 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-103490
    Takinib
    25+ 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-50759
    Ispinesib
    5+ Cited Publications

    SB-715992; CK-0238273

    		 Kinesin Apoptosis Cancer
    Ispinesib is a specific inhibitor of kinesin spindle protein (KSP), with a Ki app of 1.7 nM.
    Ispinesib
  • HY-N0192
    Arbutin
    3 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-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-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-129430
    N-Methylprotoporphyrin IX
    1 Publications Verification

    		 Ferrochelatase Metabolic Disease
    N-Methylprotoporphyrin IX is a Ferrochelatase inhibitor with a Ki app value of 3 nM. N-methylprotoporphyrin IX dimethyl ester potently inhibits the synthesis of phycocyanin and chlorophyll a. N-Methylprotoporphyrin IX can be used for the research of haem deficiency-associated disorders .
    N-Methylprotoporphyrin IX
  • HY-16009
    Buntanetap

    (+)-Phenserine; ANVS401

    		 α-synuclein Neurological Disease Inflammation/Immunology
    Buntanetap ((+)-Phenserine) is a selective acetylcholinesterase inhibitor. Buntanetap is a multiple neurotoxic protein translation inhibitor with oral activity, including amyloid precursor protein (APP), α-synuclein (αSYN) and huntingtin protein (HTT). Buntanetap reduces the production of β-amyloid precursor protein by blocking its mRNA translation. Buntanetap has anti-inflammatory effects and can be used in the study of Alzheimer's disease and Parkinson's disease .
    Buntanetap
  • HY-13438
    AZD3839 free base
    2 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-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-13769A
    TPT-260 Dihydrochloride
    2 Publications Verification

    NSC55712; TPU-260 Dihydrochloride

    		 Drug Derivative Amyloid-β Beta-secretase Cardiovascular Disease Neurological Disease Inflammation/Immunology
    TPT-260 Dihydrochloride (NSC55712), a thiophene thiourea derivative, is a retromer complex stabilizer against thermal denaturation (Kd = ~5 µM). TPT-260 Dihydrochloride increases the levels of retromer proteins, shifts amyloid-precursor protein (APP) away from the endosome, and decreases the pathogenic processing of APP. TPT-260 Dihydrochloride inhibits TLR4 upregulation, IKKβ phosphorylation, NF-κB p65 nuclear translocation, and NLRP3 inflammasome formation. TPT-260 Dihydrochloride improves retromer-mediated cargo trafficking, reduces brain infarct area, and decreases amyloid plaque deposition. TPT-260 Dihydrochloride exhibits minimal cytotoxicity to primary microglia at tested concentrations. TPT-260 Dihydrochloride can be used for the research of inflammatory bowel disease, ischemic stroke and Alzheimer's disease .
    TPT-260 Dihydrochloride
  • HY-152846
    Flizasertib

    GDC-8264

    		 RIP kinase Interleukin Related Cardiovascular Disease Inflammation/Immunology Endocrinology
    Flizasertib (GDC-8264) is an orally active, reversible and selective RIP1 inhibitor with Ki app values of 0.00071 μM and 0.0013 μM for human and cynomolgus monkey RIP1 kinase, respectively. Flizasertib blocks RIP1 autophosphorylation but does not affect RIP1 protein stability. Flizasertib inhibits pro-inflammatory cytokines (CCL3, CCL4, and IL-1β) production. Flizasertib results in inhibition of colitis and ileitis. Flizasertib can be used in the research of cardiac surgery-associated acute kidney injury .
    Flizasertib
  • HY-N1472
    Levistolide A
    5 Publications Verification

    		 Apoptosis Reactive Oxygen Species (ROS) PPAR GSK-3 Tau Protein Ras TGF-β Receptor Infection Neurological Disease Inflammation/Immunology
    Levistolide A is an apoptosis inducer and a PEDV virus inhibitor. Levistolide A can induce apoptosis in colon cancer cells and suppress the replication of porcine epidemic diarrhea virus (PEDV) by promoting ROS generation. Levistolide A activates peroxisome proliferator-activated receptor γ (PPARγ) in N2a/APP695swe cells and reduces excessive phosphorylation of tau through the GSK3α/β pathway, improving symptoms in Alzheimer’s mice. Levistolide A improves kidney damage in 5/6 nephrectomy (Nx) mice by inhibiting the RAS,TGF-β1/Smad, and MAPK pathways .
    Levistolide A
  • HY-123960
    Raphin1
    3 Publications Verification

    		 Phosphatase Neurological Disease
    Raphin1 is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease .
    Raphin1
  • HY-P5381
    gp91 ds-tat
    1 Publications Verification

    		 NADPH Oxidase Ferroptosis Reactive Oxygen Species (ROS) Glutathione Peroxidase TRP Channel Cardiovascular Disease Neurological Disease Inflammation/Immunology
    gp91 ds-tat, a biological active peptide, is a NADPH oxidase 2 (Nox2) inhibitor. gp91 ds-tat blocks NADPH oxidase-dependent superoxide production. gp91 ds-tat ameliorates high glucose-induced increase in total ROS, LPOs and iron levels. gp91 ds-tat inhibits homocysteine (Hcy)-induced activation of NLRP3 inflammasomes and restores Hcy-inhibited lysosomal TRPML1 channel activity. gp91 ds-tat improves cerebrovascular and cognitive function in APP/PS1 mice. gp91 ds-tat can be used for the study of Alzheimer’s disease (AD), glomerular inflammation and cardiovascular disease .
    gp91 ds-tat
  • HY-114174
    Fmoc-Ala-Glu-Asn-Lys-NH2
    3 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-128464
    LL320

    		Amine N-methyltransferase 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-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-103374
    Phenserine

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

    		 Cholinesterase (ChE) Amyloid-β Neurological Disease
    Phenserine ((-)-Eseroline phenylcarbamate) is a derivative of Physostigmine (HY-N6608) 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-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-126242S
    Tyk2-IN-7

    		JAK IFNAR Interleukin Related Inflammation/Immunology
    Tyk2-IN-7 is an orally active TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC50 and Ki.app of 0.00053 μM and 0.00007 μM, respectively. Tyk2-IN-7 provides a highly selective alternative to conventional TYK2 orthosteric inhibitors, inhibits TYK2/JAK1/JAK2 kinase domain. Tyk2-IN-7 can inhibit the IL-23 and IFN-α signaling pathways. Tyk2-IN-7 is commonly used in the study of inflammatory conditions such as colitis .
    Tyk2-IN-7
  • HY-123960A
    Raphin1 acetate
    3 Publications Verification

    		 Phosphatase Neurological Disease
    Raphin1 acetate is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 acetate binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 acetate crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease .
    Raphin1 acetate
  • HY-135699
    TD52
    2 Publications Verification

    		 Apoptosis Phosphatase Akt Cancer
    TD52, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 has less p-EGFR inhibition and has potent anti-cancer activity . TD52 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    TD52
  • HY-P990301
    Anti-Human/Mouse/Rat Amyloid-beta Antibody (MOAB-2)

    		Amyloid-β Neurological Disease
    Anti-Human/Mouse/Rat Amyloid-beta Antibody (MOAB-2) is a mouse-derived IgG2b λ type antibody inhibitor, targeting to Amyloid-beta. Anti-Human/Mouse/Rat Amyloid-beta Antibody (MOAB-2) recognizes unaggregated, oligomeric or fibrillar forms of Aβ42 and unaggregated Aβ40. Anti-Human/Mouse/Rat Amyloid-beta Antibody (MOAB-2) is selective for human Aβ42 over Aβ40, but not amyloid precursor protein (APP). Anti-Human/Mouse/Rat Amyloid-beta Antibody (MOAB-2) can immunostain human or rat and mouse tissue. Anti-Human/Mouse/Rat Amyloid-beta Antibody (MOAB-2) can be used for detections of western blot, immunohistochemistry, immunofluorescence, immunoprecipitation and ELISA .
    Anti-Human/Mouse/Rat Amyloid-beta Antibody (MOAB-2)
  • 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-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-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-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-401209
    Synucleozid-2.0

    		α-synuclein DNA/RNA Synthesis Neurological Disease
    Synucleozid-2.0 is a blood-brain barrier-permeable inhibitor that binds to the IRE of SNCA mRNA, with a EC50 of 2.9 µM and a Kd value of 1.8 µM. Synucleozid-2.0 selectively binds to and stabilizes the A bulge and adjacent closed base pairs in the 5' UTR IRE of SNCA mRNA, blocks the translation process and reduces intracellular levels of α-synuclein. Synucleozid-2.0 exerts cytoprotective effects against cytotoxicity induced by α-synuclein preformed fibrils. Synucleozid-2.0 is applicable to the research of Parkinson's disease .
    Synucleozid-2.0
  • 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-161723
    LH2-051

    		Dopamine Transporter CDK Neurological Disease
    LH2-051, a lysosome-enhancing compound (LYEC), is a brain-penetrant dopamine transporter (DAT) inhibitor (Ki: 0.95 μM). LH2-051 inhibits DAT-mediated dopamine uptake with an IC50 of 3.0 μM. LH2-051 promotes nuclear translocation of TFEB and lysosome biogenesis. LH2-051 improves the memory of amyloid precursor protein (APP)/Presenilin 1 (PS1) mice. LH2-051 can be used for the study of Alzheimer’s disease .
    LH2-051
  • HY-135699A
    TD52 dihydrochloride
    2 Publications Verification

    		 Akt Phosphatase Apoptosis Cancer
    TD52 dihydrochloride, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 dihydrochloride mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 dihydrochloride indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 dihydrochloride has less p-EGFR inhibition and has potent anti-cancer activity . TD52 (dihydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    TD52 dihydrochloride
  • HY-N3001
    Isolinderalactone
    1 Publications Verification

    		 STAT VEGFR Bcl-2 Family Survivin IAP NF-κB Apoptosis Caspase Neurological Disease Inflammation/Immunology Cancer
    Isolinderalactone is a sesquiterpene that exhibits anti-cancer, anti-inflammatory, and neuroprotective effects. Isolinderalactone inhibits VEGF expression and tyrosine phosphorylation of VEGFR2. Isolinderalactone decreases viability and induces apoptosis in U-87 glioblastoma (GBM) cells and colorectal cancer (CRC) cells. Isolinderalactone induces G2/M phase cell cycle arrest, ROS generation, pJNK/p38 MAPK activation, in colorectal cancer (CRC) cells. Isolinderalactone blocks LPS (HY-D1056)-induced NF-κB activation while activating Nrf2-HMOX1 signaling in RAW264.7 macrophages. Isolinderalactone improves cognitive dysfunction in APP/PS1 mice. Isolinderalactone can be used for the study of Glioblastoma multiforme (GBM), colorectal cancer, Alzheimer’s disease and acute lung injury .
    Isolinderalactone
  • 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-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-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-169296
    IMPDH2-IN-4

    		IMPDH Cancer
    IMPDH2-IN-4 (Compound 2d) is a selective IMPDH2 inhibitor with a Ki,app value of 1.8 μM. IMPDH2-IN-4 exhibits anti-cancer activity against osteosarcoma. IMPDH2-IN-4 can be used in research related to osteosarcoma .
    IMPDH2-IN-4
  • HY-N1414A
    3′,6-Disinapoylsucrose
    2 Publications Verification

    		 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-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-174367
    RUNX1/ETO-IN-1

    		RUNX Apoptosis Cancer
    RUNX1/ETO-IN-1 is a RUNX1-ETO oncogenic fusion protein inhibitor that specifically targets the NHR2 oligomerization domain. RUNX1/ETO-IN-1 directly interacts with the NHR2 (KD,app = 39 μM). RUNX1/ETO-IN-1 exhibits anti-leukemic activity by inducing apoptosis and promoting differentiation in RUNX1/ETO-translocated AML cells. RUNX1/ETO-IN-1 remains essentially uncharged at physiological pH, demonstrating superior membrane permeability.
    RUNX1/ETO-IN-1
  • 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-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-121817
    Sulfiram

    		Aldehyde Dehydrogenase (ALDH) Drug Intermediate Amyloid-β Infection Neurological Disease
    Sulfiram is a very weak aldehyde dehydrogenase (ALDH) inhibitor, with an IC50 value of 413 μM against Saccharomyces cerevisiae ALDH. As a photochemical precursor, Sulfiram undergoes photoconversion to form Disulfiram (HY-B0240), a potent ALDH inhibitor. Sulfiram inhibits the dimerization of the extracellular domain fragment (amino acid residues 230-624) of amyloid precursor protein (APP), alters the monomer-dimer equilibrium, induces conformational changes in the fragment, and enhances the production of sAPPα via α-cleavage of APP. Sulfiram can be used in research related to scabies and Alzheimer's disease .
    Sulfiram
  • HY-176271
    MAO-B-IN-45

    		Ferroptosis Monoamine Oxidase Glutathione Peroxidase Reactive Oxygen Species (ROS) Tau Protein Amyloid-β Neurological Disease
    MAO-B-IN-45 is a dual inhibitor of ferroptosis and MAO-B. MAO-B-IN-45 shows selectivity towards MAO-B with an IC50 of 87.47 nM and selectivity exceeding 229-fold for MAO-B over MAO-A. MAO-B-IN-45 has excellent antiferroptosis activity through modulation of the iron metabolic pathway and GSH-GPX4 axis in vitro. MAO-B-IN-45 improves cognitive and behavioral impairments in 3×Tg (APP/Tau/Ps1) AD mouse and significantly reduced the levels of ferritin heavy chain 1 (FTH1), APP, and Tau phosphorylation (p-Tau) proteins in the brain.
    MAO-B-IN-45
  • 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-16009B
    Buntanetap L-Tartrate

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

    		 Amyloid-β Neurological Disease
    Buntanetap L-Tartrate (Phenserine L-Tartrate) is a selective AChE inhibitor (IC50 = 22.2 nM). Buntanetap is a multiple neurotoxic protein translation inhibitor with oral activity, including amyloid precursor protein (APP), α-synuclein (αSYN) and huntingtin protein (HTT). Buntanetap reduces the production of β-amyloid precursor protein by blocking its mRNA translation. Buntanetap has anti-inflammatory effects and can be used in the study of Alzheimer's disease and Parkinson's disease .
    Buntanetap L-Tartrate

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