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aminopeptidase inhibitor

" in MedChemExpress (MCE) Product Catalog:

102

Inhibitors & Agonists

6

Peptides

16

Natural
Products

2

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B0134
    Bestatin
    Maximum Cited Publications
    11 Publications Verification

    Ubenimex

    		 Aminopeptidase Bacterial Antibiotic Infection Cancer
    Bestatin is a natural, broad-spectrum, and competitive CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase inhibitor. Bestatin has anticancer effects .
    Bestatin
  • HY-15695
    Puromycin aminonucleoside
    Maximum Cited Publications
    37 Publications Verification

    NSC 3056

    		 Bacterial Apoptosis Dipeptidyl Peptidase Aminopeptidase Antibiotic Infection Inflammation/Immunology Cancer
    Puromycin aminonucleoside (NSC 3056) is the aminonucleoside portion of the antibiotic puromycin, and used in nephrosis animal models . Puromycin aminonucleoside induces apoptosis . Puromycin aminonucleoside is a reversible inhibitor of dipeptidyl peptidase II and cytosol alanyl aminopeptidase . Puromycin aminonucleoside induces secretion of cell migrasome .
    Puromycin aminonucleoside
  • HY-B0134A
    Bestatin hydrochloride
    Maximum Cited Publications
    11 Publications Verification

    Ubenimex hydrochloride

    		 Antibiotic Bacterial Aminopeptidase Infection Cancer
    Bestatin hydrochloride is an inhibitor of CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase, used for cancer research.
    Bestatin hydrochloride
  • HY-14807
    Tosedostat
    5+ Cited Publications

    CHR-2797

    		 Aminopeptidase Cancer
    Tosedostat (CHR-2797) is an orally active aminopeptidase inhibitor. CHR-2797 exerts antiproliferative effects against a range of tumor cell lines .
    Tosedostat
  • HY-113952
    Actinonin
    5+ Cited Publications

    (-)-Actinonin

    		 Aminopeptidase Bacterial MMP Apoptosis Antibiotic Infection Cancer
    Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities .
    Actinonin
  • HY-115194
    Amastatin hydrochloride
    1 Publications Verification

    		 Aminopeptidase Bacterial Infection
    Amastatin hydrochloride is a slow, tight binding, competitive aminopeptidase (AP) inhibitor with Ki values of 0.26 nM, 30 nM, 52 nM for Aeromonas aminopeptidase, cytosolic leucine aminopeptidase, microsomal aminopeptidase .
    Amastatin hydrochloride
  • HY-133125
    ERAP1-IN-1
    5 Publications Verification

    		 Aminopeptidase Inflammation/Immunology
    ERAP1-IN-1 is an endoplasmic reticulum aminopeptidase 1 (ERAP1) inhibitor. ERAP1-IN-1 competitively inhibits ERAP1 activity towards a nonamer peptide representative of physiological substrates .
    ERAP1-IN-1
  • HY-B1467
    Domiphen bromide
    1 Publications Verification

    		 Potassium Channel Bacterial Parasite Phosphatase Infection Inflammation/Immunology
    Domiphen bromide is a cationic active quaternary ammonium salt and also an inhibitor of HERG channels (IC50: 9 nM), aminopeptidase-like enzymes, Escherichia coli alkaline phosphatase, and α-chymotrypsin. Domiphen bromide has multiple activities such as antibacterial, antimalarial, and disinfectant properties, and it is also a synergist of Colistin (HY-113678). Domiphen bromide can be used as a chemical preservative and a cationic surfactant, and it can also be used in the research of bacterial infectious diseases such as pharyngitis, thrush, and oral ulcers .
    Domiphen bromide
  • HY-147257
    Cofrogliptin

    HSK7653

    		 Dipeptidyl Peptidase Metabolic Disease
    Cofrogliptin (HSK7653) (compound 2), a tetrahydropyran derivative, is a potent oral dipeptidyl aminopeptidase 4 (DPP-4) inhibitor with Long-acting antidiabetic efficacy. Cofrogliptin (compound 2) has a great potential for type 2 diabetes mellitus (T2DM) .
    Cofrogliptin
  • HY-101932
    TNP-470
    2 Publications Verification

    AGM-1470

    		 Aminopeptidase Cardiovascular Disease Cancer
    TNP-470 is a methionine aminopeptidase-2 inhibitor and also an angiogenesis inhibitor.
    TNP-470
  • HY-W345510
    Opiorphin

    		Neprilysin Neurological Disease
    Opiorphin, an opioid peptide, is a potent enkephalin-inactivating zinc ectopeptidases in human inhibitor. Opiorphin inhibits two enkephalin-catabolizing ectoenzymes, human neutral ecto-endopeptidase, hNEP (EC 3.4.24.11) with an IC50 value of 11 μM, and human ecto-aminopeptidase, hAP-N (EC 3.4.11.2). Opiorphin displays potent analgesic activity by activating endogenous opioid-dependent transmission .
    Opiorphin
  • HY-151518
    Aminopeptidase-IN-1

    		Aminopeptidase Neurological Disease
    Aminopeptidase-IN-1 is an insulin-regulated aminopeptidase (IRAP) inhibitor with an Ki value of 7.7 μM. Aminopeptidase-IN-1 can be used for the research of memory impairments .
    Aminopeptidase-IN-1
  • HY-133016
    M8891

    		MetAP Cardiovascular Disease Cancer
    M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor with an IC50 of 54 nM and a Ki of 4.33 nM. M8891 does not inhibit MetAP-1 (IC50>10 µM) . M8891 inhibits growth of primary endothelial cells as well as tumor cells and demonstrates antiangiogenic and antitumoral activity .
    M8891
  • HY-W015876
    L-Leucinol

    (+)-Leucinol

    		 Aminopeptidase Others
    L-Leucinol ((+)-Leucinol) is a competitive aminopeptidase inhibitor with a Ki value of 17 μM. As a dietary intake inhibitor, L-Leucinol reduces the basal dietary leucine intake in rats via microinjection into the rat anterior piriform cortex .
    L-Leucinol
  • HY-109058
    Firibastat
    1 Publications Verification

    QGC001; RB150

    		 Aminopeptidase Cardiovascular Disease Neurological Disease
    Firibastat (QGC001), an orally active brain penetrating proagent of EC33, is a first-in-class brain aminopeptidase A (APA) inhibitor (Ki=200 nM). Firibastat selectively and specifically inhibits conversion of brain angiotensin-II into angiotensin-III and decreases blood pressure in hypertensive rats .
    Firibastat
  • HY-120868
    TP-004
    1 Publications Verification

    		 MetAP Metabolic Disease Cancer
    TP-004 is a potent and reversible inhibitor of methionine aminopeptidase 2 (MetAP2), with an IC50 of 6 nM against MetAP2. TP-004 is a chemical probe. TP-004 suppresses MetAP2 enzymatic activity, blocks N-terminal methionine cleavage, impairs protein maturation and stability, and thereby inhibits cell proliferation and angiogenesis. TP-004 can be used for the study of tumors and diseases associated with excessive angiogenesis .
    TP-004
  • HY-13731
    PPI-2458

    		MetAP Inflammation/Immunology Cancer
    PPI-2458 is a potent, orally active, selective and irreversible inhibitor of methionine aminopeptidase-2 (MetAP-2). PPI-2458 can be used for arthritis and lymphoma research .
    PPI-2458
  • HY-W027340
    ARM1
    1 Publications Verification

    4BSA

    		 Aminopeptidase Epoxide Hydrolase Cancer
    ARM1 (4BSA) is a potent aminopeptidase and epoxide hydrolase inhibitor. ARM1 shows aminopeptidase inhibitory activity with an IC50 7.61 µM and epoxide hydrolase inhibitory activity with an IC50 12.4 µM .
    ARM1
  • HY-148442
    ecMetAP-IN-1

    		MetAP Bacterial Infection
    ecMetAP-IN-1 is an inhibitor of E. coli methionine aminopeptidase (ecMetAP) with an IC50 of 2.086 μM. ecMetAP-IN-1 is applicable to research related to bacterial infections caused by E. coli .
    ecMetAP-IN-1
  • HY-177590
    14-3-3-IN-2

    		MMP Others
    14-3-3-IN-2 is a 14-3-3 protein inhibitor with an IC50 of 15 nM. 14-3-3-IN-2 can disrupt the interaction of 14-3-3α with aminopeptidase N and down-regulate 14-3-3α increased MMP-1 mRNA levels .
    14-3-3-IN-2
  • HY-14811
    Beloranib

    ZGN-440; CKD-732 free base

    		 MetAP NF-κB Metabolic Disease
    Beloranib (ZGN-440; CKD-732 free base) is a selective, irreversible inhibitor of methionine aminopeptidase MetAP2 that suppresses appetite and increases energy expenditure. Beloranib blocks the enzymatic cleavage of N-terminal methionine from nascent proteins by forming a covalent bond with MetAP2, thereby regulating fatty acid metabolism, adrenergic signaling, and hypothalamic NF-κB expression. Beloranib significantly reduces food intake, body weight, and fat accumulation, while improving glucose tolerance, insulin sensitivity, and lipid metabolism. Beloranib also elevates energy expenditure and fat oxidation levels, without affecting body temperature, spontaneous activity, or the inflammatory cytokine IL-1β. Beloranib can be used in research on obesity and hypothalamic obesity .
    Beloranib
  • HY-147401
    Sitagliptin fenilalanil
    1 Publications Verification

    		 Dipeptidyl Peptidase Metabolic Disease
    Sitagliptin fenilalanil is a dipeptidyl aminopeptidase 4 (DPP-4) inhibitor .
    Sitagliptin fenilalanil
  • HY-110259
    HFI-142
    1 Publications Verification

    		 Aminopeptidase Neurological Disease
    HFI-142 is an insulin-regulated aminopeptidase (IRAP) inhibitor with a Ki of 2.01 μM .
    HFI-142
  • HY-W011539
    EcMetAP1-IN-1

    		Bacterial Infection
    EcMetAP1-IN-1 (compound 4) is an inhibitor of Escherichia coli methionine aminopeptidase MetAP1 .
    EcMetAP1-IN-1
  • HY-B0134AS
    Bestatin-d7 hydrochloride

    Ubenimex-d7 hydrochloride

    		 Isotope-Labeled Compounds Aminopeptidase Bacterial Antibiotic Infection Cancer
    Bestatin-d7 (hydrochloride) is deuterium labeled Bestatin (hydrochloride). Bestatin hydrochloride is an inhibitor of CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase, used for cancer research.
    Bestatin-d7 hydrochloride
  • HY-111173
    Diprotin B

    		Dipeptidyl Peptidase Others
    Diprotin B is a dipeptidyl aminopeptidase IV (DPP IV) inhibitor. The apparent competitive inhibition of DPP-IV by the diprotins is a kinetic artifact, derived from the substrate-like nature of tripeptides containing a penultimate proline residue .
    Diprotin B
  • HY-118953
    LAF389

    		MetAP Drug Intermediate Cancer
    LAF389, a prodrug of LAF153 (HY-183876), is a methionine aminopeptidase (MetAps) inhibitor with an IC50 of 800 nM against MetAp2, and exhibits a maximum inhibition rate of 20% against MetAp1 at 300 nM. LAF389 possesses antiproliferative, antiangiogenic and cytotoxic activities. LAF389 can be used in research related to cancers such as advanced solid tumors .
    LAF389
  • HY-P1044
    Spinorphin

    LVV-hemorphin-4

    		 Carboxypeptidase Neurological Disease
    Spinorphin is an inhibitor of enkephalin-degrading enzymes. Spinorphin inhibits aminopeptidase, dipeptidyl aminopeptidase III, angiotensin-converting enzyme and enkephalinase. Spinorphin possesses an antinociceptive effect .
    Spinorphin
  • HY-P1044A
    Spinorphin TFA

    LVV-hemorphin-4 TFA

    		 Angiotensin Receptor Neurological Disease
    Spinorphin TFA is an inhibitor of enkephalin-degrading enzymes. Spinorphin inhibits aminopeptidase, dipeptidyl aminopeptidase III, angiotensin-converting enzyme and enkephalinase. Spinorphin possesses an antinociceptive effect .
    Spinorphin TFA
  • HY-133016A
    (R)-M8891

    		MetAP Others
    (R)-M8891 (compound R-9) is a less active isomer of M8891. M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor .
    (R)-M8891
  • HY-122369
    Histargin

    		Carboxypeptidase Metabolic Disease
    Histargin is a selective carboxypeptidase B inhibitor with an IC50 of 17 μg/mL and a Ki of 30 μM. Histargin exerts competitive inhibition with substrate, with inhibitory activity abolished by metal cations. Histargin shows no significant inhibitory activity against carboxypeptidase A, aminopeptidase A, or aminopeptidase B .
    Histargin
  • HY-160239
    HFI-437

    		Aminopeptidase Neurological Disease
    HFI-437 is a potent non-peptidic insulin-regulated aminopeptidase (IRAP) inhibitor with a Ki of 20 nM. HFI-437 is a cognitive enhancer .
    HFI-437
  • HY-109188
    Relzomostat

    		MetAP Metabolic Disease
    Relzomostat is a methionine aminopeptidase 2 (MetAP2) inhibitor.Relzomostat may be useful for the research of obesity, type 2 diabetes, and other obesity-associated conditions .
    Relzomostat
  • 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-158006
    SDX-7539

    		MetAP Cancer
    SDX-7539 is a selective inhibitor for Methionine aminopeptidase type 2 (MetAP2). SDX-7539 inhibits proliferarion of HUVECs with an IC50 of 120 μM. SDX-7539 exhibits antitumor activity in NSCLC xenograft athymic nude mice .
    SDX-7539
  • HY-126564
    Ebelactone A

    		Lipase MetAP Others Inflammation/Immunology
    Ebelactone A is a mycolic acid β-lactone, which exhibits inhibitory activity for esterase, lipase, fMet aminopeptidase (fMet AP) and PNBase, with IC50s of 56, 3, 8 and 7.5 μM, respectively . Ebelactone A inhibits cutinase, exhibits plants protective potency against Erysiphe graminis .
    Ebelactone A
  • HY-117702
    RB 101

    		Prolyl Endopeptidase (PREP) Aminopeptidase Opioid Receptor Dopamine Receptor Drug Intermediate Neurological Disease Metabolic Disease Inflammation/Immunology
    RB 101 is a blood-brain barrier-crossing prodrug as well as aminopeptidase N and neutral endopeptidase-24.11 inhibitor. RB 101 blocks enkephalin breakdown, elevates extracellular enkephalin levels and activate δ-opioid receptor and dopamine D1 receptor. RB 101 can be used for the research of pain, depressive syndromes, and diabetic neuropathy .
    RB 101
  • HY-N2150
    Psammaplin A

    		HDAC DNA Methyltransferase DNA/RNA Synthesis Bacterial Aminopeptidase Farnesyl Transferase PPAR Apoptosis Infection Inflammation/Immunology Cancer
    Psammaplin A is a marine metabolite. Psammaplin A is a selective HDAC1 (IC50: 45 nM), DNA methyltransferases (IC50: 18.6 nM) and aminopeptidase N (APN) (IC50: 18 μM) inhibitor. Psammaplin A also inhibits DNA topoisomerase and farnesyl protein transferase. Psammaplin A is a PPARγ activator and induces apoptosis. Psammaplin A has antitumor and anti-inflammatory activities. Psammaplin A has antibacterial activity against Gram-positive bacteria and inhibits DNA synthesis and DNA gyrase activity. Psammaplin A inhibits angiogenesis .
    Psammaplin A
  • HY-19876
    PL37

    Debio-0827

    		 Opioid Receptor Aminopeptidase Neprilysin Neurological Disease Metabolic Disease
    PL37 (Debio-0827) is an orally active Enkephalinase dual inhibitor (dual inhibition refers to the simultaneous inhibition of Neutral Endopeptidase and Aminopeptidase N activities). PL37 exerts its anti-hyperalgesic effects by activating μ-opioid receptors (µ-opioid receptors), with an ED50 value of 13.4 mg/kg for analgesic effects in mice. PL37 can be used to study diabetic neuropathic pain .
    PL37
  • HY-14811A
    Beloranib hemioxalate

    ZGN-440 hemioxalate; ZGN-433 hemioxalate; CDK732 hemioxalate

    		 NF-κB MetAP Metabolic Disease
    Beloranib (ZGN-440; CKD-732 free base) hemioxalate is a selective, irreversible inhibitor of methionine aminopeptidase MetAP2 that suppresses appetite and increases energy expenditure. Beloranib hemioxalate blocks the enzymatic cleavage of N-terminal methionine from nascent proteins by forming a covalent bond with MetAP2, thereby regulating fatty acid metabolism, adrenergic signaling, and hypothalamic NF-κB expression. Beloranib hemioxalate significantly reduces food intake, body weight, and fat accumulation, while improving glucose tolerance, insulin sensitivity, and lipid metabolism. Beloranib hemioxalate also elevates energy expenditure and fat oxidation levels, without affecting body temperature, spontaneous activity, or the inflammatory cytokine IL-1β. Beloranib hemioxalate can be used in research on obesity and hypothalamic obesity .
    Beloranib hemioxalate
  • HY-147401A
    Sitagliptin fenilalanil hydrochloride
    1 Publications Verification

    		 Dipeptidyl Peptidase Metabolic Disease
    Sitagliptin fenilalanil hydrochloride is a dipeptidyl aminopeptidase 4 (DPP-4) inhibitor .
    Sitagliptin fenilalanil hydrochloride
  • HY-137159
    Bestatin methyl ester

    		Aminopeptidase Ligands for Target Protein for PROTAC IAP Cancer
    Bestatin methyl ester is a cell permeable Zn2+-binding aminopeptidases inhibitor. Bestatin methyl ester inhibits spore cell differentiation .
    Bestatin methyl ester
  • HY-P11334
    Cyanostatin B

    		Aminopeptidase Phosphatase Angiotensin-converting Enzyme (ACE) DNA/RNA Synthesis Cancer
    Cyanostatin B, a cyanobacterial lipopeptide, is a leucine aminopeptidase M (LAP) inhibitor (IC50 = 12 ng/mL). Cyanostatin B is a weak inhibitor of protein phosphatase (PP2A) and also exhibits weak inhibitory activity against angiotensin-converting enzyme (ACE), with an IC50 value of 130 μg/mL. Cyanostatin B demonstrates both cytotoxic and genotoxic effects on human hepatocytes, although non-toxic to Artemia salina. Cyanostatin B inhibits the proliferation of HepG2 cells, induces DNA single-strand breaks, and causes genomic instability. .
    Cyanostatin B
  • HY-129298
    Amastatin

    		Aminopeptidase Others
    Amastatin is A slow, tightly bound, competitive inhibitor of aminopeptidase (AP) with an IC50 of 0.54 μg/mL for AP-A .
    Amastatin
  • HY-N9898
    Sinocrassoside C1

    		Others Others
    Sinocrassoside C1 is a natural compound isolated from themethanolic extract of the whole plant ofSinocrassula indica (Crassulaceae) .
    Sinocrassoside C1
  • HY-W012888
    D-Leucinol

    (-)-Leucinol

    		 Aminopeptidase Others
    D-Leucinol is the isomer of L-Leucinol (HY-W015876), and can be used as an experimental control. L-Leucinol ((+)-Leucinol) is a competitive aminopeptidase inhibitor with Ki value of 17 μM .
    D-Leucinol
  • HY-162920
    QGC583

    		Aminopeptidase Cardiovascular Disease
    QGC583 is an effective selective Aminopeptidase A (APA) inhibitor with oral activity and blood-brain barrier permeability, boasting an IC50 value of 4 nM. QGC583 can inhibit APA activity in the brain, kidneys, and heart of rats .
    QGC583
  • HY-116126
    Leuhistin

    		Aminopeptidase Cancer
    Leuhistin is an AP-M (aminopeptidase-M) inhibitor. AP-M is an inactivating enzyme of bioactive peptides in cerebral membranes. Leuhistin can be produced by Bacillus laterosporus BMI156-14F1 .
    Leuhistin
  • HY-B0134R
    Bestatin (Standard)

    Ubenimex (Standard)

    		 Reference Standards Aminopeptidase Bacterial Antibiotic Infection Cancer
    Bestatin (Standard) is the analytical standard of Bestatin. This product is intended for research and analytical applications. Bestatin is a natural, broad-spectrum, and competitive CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase inhibitor. Bestatin has anticancer effects .
    Bestatin (Standard)
  • HY-163727
    MMV1557817

    		Parasite Infection
    MMV1557817 is an orally active and potent antimalarial compound. MMV1557817 is a selective, nanomolar inhibitor of both Plasmodium falciparum and Plasmodium vivax aminopeptidases M1 and M17, leading to inhibition of end-stage hemoglobin digestion in asexual parasites .
    MMV1557817

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