2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Aminopeptidase

Aminopeptidase

Aminopeptidase

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Aminopeptidases catalyze the cleavage of amino acids from the amino terminus of protein or peptide substrates. Regarding catalytic mechanism, most of the aminopeptidases are metallo-enzymes but cysteine and serine peptidases are also included in this group. Aminopeptidases are widely distributed throughout the animal and plant kingdoms and are found in many subcellular organelles, in cytoplasm, and as membrane components. Several aminopeptidases perform essential cellular functions. Many, but not all, of these peptidases are zinc metalloenzymes and are inhibited by the transition-state analog bestatin. Some are monomeric, and others are assemblies of relatively high mass (50 kDa) subunits.

Functional roles of the angiotensin peptides of the renin-angiotensin system (RAS) cascade can be analyzed through their corresponding proteolytic regulatory enzymes aspartyl aminopeptidase (ASAP), aminopeptidase A (APA), aminopeptidase B (APB), aminopeptidase N (APN) and insulin-regulated aminopeptidase (IRAP). These enzyme activities generate active or inactive angiotensin peptides that alter the ratios between their bioactive forms, regulating several important processes such as the regulation of cardiovascular functions, body water regulation, normal memory consolidation and retrieval, but also cell growth, differentiation and apoptosis or the inflammatory response.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-15695
    Puromycin aminonucleoside
    		Inhibitor 99.90%
    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-B0134
    Bestatin
    		Inhibitor 99.97%
    Bestatin is a natural, broad-spectrum, and competitive CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase inhibitor. Bestatin has anticancer effects.
    Bestatin
  • HY-113952
    Actinonin
    		Inhibitor 98.61%
    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-B0134A
    Bestatin hydrochloride
    		Inhibitor 99.94%
    Bestatin hydrochloride is an inhibitor of CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase, used for cancer research.
    Bestatin hydrochloride
  • HY-101932
    TNP-470
    		Inhibitor 99.87%
    TNP-470 is a methionine aminopeptidase-2 inhibitor and also an angiogenesis inhibitor.
    TNP-470
  • HY-19876
    PL37
    		Antagonist
    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-10826
    DG051 free acid
    		Inhibitor
    DG051 (free acid) is an effective inhibitor of leukotriene A4 hydrolase (LTA4H), with a Kd of 26 nM. It has high water solubility (greater than 30 mg/mL) and high oral bioavailability (over 80% across different species). DG051 (free acid) can be used in research related to myocardial infarction and stroke.
    DG051 free acid
  • HY-118661
    BDM14471
    		Inhibitor
    BDM14471 is a selective inhibitor of hydroxamate aminopeptidase M1 (PfAM1), with the IC50 of 6 nM.
    BDM14471
  • HY-B0494
    Bufexamac
    		Inhibitor ≥98.0%
    Bufexamac is a selective Ⅱb HDAC (HDAC6, HDAC10) and LTA4H dual inhibitor, with Kds of 0.53 µM and 0.22 µM for HDAC6 and HDAC10. Bufexamac is a nonsteroida anti-inflammatory drug.
    Bufexamac
  • HY-103226
    SC-57461A
    		Inhibitor 99.89%
    SC-57461A is a potent, orally active, nonpeptide, and selective inhibitor of Leukotriene A4 (LTA4) hydrolase with IC50s of 2.5 nM, 3 nM, and 23 nM for recombinant human, mouse, and rat LTA4 hydrolase, respectively.
    SC-57461A
  • HY-14807
    Tosedostat
    		Inhibitor 99.75%
    Tosedostat (CHR-2797) is an orally active aminopeptidase inhibitor. CHR-2797 exerts antiproliferative effects against a range of tumor cell lines.
    Tosedostat
  • HY-109058
    Firibastat
    		Inhibitor ≥98.0%
    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-P1043A
    NGR peptide Trifluoroacetate
    		98.06%
    NGR peptide Trifluoroacetatecontaining the Asn-Gly-Arg (NGR) motif. NGR peptide Trifluoroacetate binds to APN/CD13. NGR peptide Trifluoroacetate is directly conjugated to imaging agents that can be used for tumor imaging.
    NGR peptide Trifluoroacetate
  • HY-137298
    LYS006
    		Inhibitor 98.61%
    LTA4H-IN-1 is a potent inhibitor of leukotriene A4 hydrolase (LTA4H) extracted from patent WO2015092740A1, example 29, has an IC50 of 2 nM. LTA4H-IN-1 can be used for the research of inflammatory and autoimmune disorders.
    LYS006
  • HY-150504
    ERAP2-IN-1
    		Inhibitor 98.86%
    ERAP2-IN-1 (compound 61) is an uncompetitive ERAP2 inhibitor. ERAP2-IN-1 specifically inhibits the ERAP2 peptide hydrolysis activity, inhibiting Arg-AMC hydrolysis with an IC50 of 27 μM and model peptide hydrolysis with an IC50 of 44 μM.
    ERAP2-IN-1
  • HY-110259
    HFI-142
    		Inhibitor 99.55%
    HFI-142 is an insulin-regulated aminopeptidase (IRAP) inhibitor with a Ki of 2.01 μM.
    HFI-142
  • HY-W015876
    L-Leucinol
    		Inhibitor 99.53%
    L-Leucinol ((+)-Leucinol) is a competitive aminopeptidase inhibitor with Ki value of 17 μM.
    L-Leucinol
  • HY-160239
    HFI-437
    		Inhibitor 99.64%
    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-151518
    Aminopeptidase-IN-1
    		Inhibitor 98.02%
    Aminopeptidase-IN-1 (compound 16o) is a potent insulin-regulated aminopeptidase (IRAP) inhibitor with an Ki value of 7.7 μM. Aminopeptidase-IN-1 can be used tor research cognitive and memory impairments.
    Aminopeptidase-IN-1
  • HY-W027340
    ARM1
    		Inhibitor 99.60%
    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
Cat. No. Product Name / Synonyms Application Reactivity