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Aminopeptidase

Aminopeptidases are enzymes that catalyze the cleavage of amino acids from the amino terminus (N-terminus) of proteins or peptides (exopeptidases).They are widely distributed throughout the animal and plant kingdoms and are found in many subcellular organelles, in cytosol, and as membrane components. Aminopeptidases are used in essential cellular functions. Many, but not all, of these peptidases are zinc metalloenzymes.Some aminopeptidases are monomeric, and others are assemblies of relatively high mass (50 kDa) subunits. cDNA sequences are available for several aminopeptidases and a crystal structure of the open state of human endoplasmic reticulum Aminopeptidase 1 ERAP1 is presented here. Amino acid sequences determined directly or deduced from cDNAs indicate some amino acid sequence homologies in organisms as diverse as Escherichia coli and mammals, particularly in catalytically important residues or in residues involved in metal ion binding.

  • α-Cyclopentyl-4-(2-quinolinylmethoxy)benzeneacetic acid
    T60040128253-12-3In house
    α-Cyclopentyl-4-(2-quinolinylmethoxy)benzeneacetic acid was identified as possible dual inhibitors for hLTA4H and hLTC4S enzymes by the computer-aided methodology.
    • $117
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  • SC-22716
    T28698262451-89-8
    SC-22716 is an orally active leukotriene A4 (LTA4) hydrolase inhibitor.SC-22716 has potential anti-inflammatory activity and may be used in the study of inflammatory bowel disease and psoriasis.
    • $293
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    TargetMol | Inhibitor Sale
  • Bestatin
    T125758970-76-6
    Bestatin (Ubenimex) competitively inhibits many aminopeptidases, including B, N and leucine aminopeptidases. Ubenimex is a microbial metabolite and dipeptide with potential immunomodulatory and antitumor activities. Aminopeptidases has been implicated in the process of cell adhesion and invasion of tumor cells. Therefore, inhibiting aminopeptidases may partially attribute to the antitumor effect of ubenimex. This agent also activates T lymphocyte, macrophage, and bone marrow stem cell as well as stimulates the release of interleukin-1 and -2, thus further enhances its antitumor activity.
    • $48
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    TargetMol | Citations Cited
  • Betulinic acid
    T2830472-15-1
    Betulinic acid (ALS-357) is a pentacyclic lupane-type triterpene derivative of betulin (isolated from the bark of Betula alba, the common white birch) which has antiretroviral, antimalarial, and anti-inflammatory properties, as well as a more recently discovered potential as an anticancer agent, by inhibition of topoisomerase.
    • $33
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  • Bestatin hydrochloride
    T352965391-42-6
    Bestatin hydrochloride (Ubenimex hydrochloride) is an inhibitor of aminopeptidase N (APN)/CD13 and aminopeptidase B.
    • $47
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    TargetMol | Citations Cited
  • ARM1
    T2185968729-05-5
    ARM1 is a potent inhibitor of aminopeptidase and epoxide hydrolase. The IC50 values are 7.61 µM for aminopeptidase and 12.4 µM for epoxide hydrolase.
    • $32
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  • Firibastat
    T28482648927-86-0
    Firibastat (RB150) is a glutamyl aminopeptidase antagonist and an orally active brain penetrating prodrug of EC33. It is a first-in-class brain aminopeptidase A (APA) inhibitor with a Ki of 200 nM. Firibastat selectively and specifically inhibits conversion of brain angiotensin-II into angiotensin-III and decreases blood pressure in hypertensive rats[1][2].
    • $41
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  • Acebilustat
    T3715943764-99-6
    Acebilustat (CTX-4430) (ZK322) is an effective and specific leukotriene B4 hydrolase inhibitor.
    • $38
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  • Actinonin
    T1412113434-13-4
    Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces and a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM, it also is an apoptosis inducer. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase, it 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 has antiproliferative and antitumor activities[1][2][3][4][5].
      7-10 days
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    • Aminopeptidase-IN-1
      T61278374102-08-6
      Aminopeptidase-IN-1 is a potent inhibitor of insulin-regulated aminopeptidase (IRAP) (Ki: 7.7 μM).Aminopeptidase-IN-1 can be used in studies of cognitive and memory disorders.
      • $39
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    • DG051
      TQ0047929915-58-2
      DG051 is a potent leukotriene A4 hydrolase (LTA4H) inhibitor (IC50: 47 nM).
      • $48
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    • Tosedostat
      T6301238750-77-1
      Tosedostat (CHR-2797) is an orally bioavailable inhibitor of the M1 family of aminopeptidases with potential antineoplastic activity. Tosedostat is converted intracellularly into a poorly membrane-permeable active metabolite (CHR-79888) which inhibits the M1 family of aminopeptidases, particularly puromycin-sensitive aminopeptidase (PuSA), and leukotriene A4 (LTA4) hydrolase; inhibition of these aminopeptidases in tumor cells may result in amino acid deprivation, inhibition of protein synthesis due to a decrease in the intracellular free amino acid pool, an increase in the level of the proapoptotic protein Noxa, and cell death.
      • $50
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    • SC-57461A
      T21696423169-68-0
      SC 57461A is a potent and specific leukotriene A4 hydrolase (LTA4H) inhibitor.
      • $41
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    • L(+)-Leucinol
      T56527533-40-6
      L(+)-Leucinol is a potent inhibitor of leucine aminopeptidase.
      • $47
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    • Puromycin aminonucleoside
      T1668458-60-6
      Puromycin aminonucleoside (NSC-3056) increases podocyte permeability by modulating ZO-1 in an oxidative stress-dependent manner.
      • $39
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    • Methyl arachidate
      T79581120-28-1
      Methyl arachidate (Methyl Icosanoate) is an esterified form of arachidic acid
      • $29
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