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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.

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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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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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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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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Acebilustat
T3715943764-99-6
Acebilustat (CTX-4430) (ZK322) is an effective and specific leukotriene B4 hydrolase inhibitor.
  • $32
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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. Intracellularly converted into the poorly membrane-permeable active metabolite (CHR-79888), it inhibits puromycin-sensitive aminopeptidase (PuSA) and leukotriene A4 (LTA4) hydrolase. This inhibition in tumor cells may lead to amino acid deprivation, suppressed protein synthesis, increased proapoptotic protein Noxa levels, and ultimately, cell death.
  • $50
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DG051
TQ0047929915-58-2
DG051 is a potent leukotriene A4 hydrolase (LTA4H) inhibitor with an IC50 of 47 nM.
  • $31
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SC-57461A
T21696423169-68-0
SC 57461A is a potent and specific leukotriene A4 hydrolase (LTA4H) inhibitor.
  • $35
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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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L(+)-Leucinol
T56527533-40-6
L(+)-Leucinol is a potent inhibitor of leucine aminopeptidase.
  • $30
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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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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.
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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 induces apoptosis and inhibits aminopeptidase M, aminopeptidase N, and leucine aminopeptidase, as well as MMP-1, MMP-3, MMP-8, MMP-9, and meprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin exhibits antiproliferative and antitumor activities [1][2][3][4][5].
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    QGC583
    T2006212417001-25-1
    QGC583 is an effective and selective AminopeptidaseA (APA) inhibitor, demonstrating an IC50 of 4 nM. It inhibits APA activity in the brain, kidneys, and heart of rats.
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    10-14 weeks
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