aminopeptidase a

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].

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.

L(+)-Leucinol is a potent inhibitor of leucine aminopeptidase.

TNP-470 is a methionine aminopeptidase-2 inhibitor and an angiogenesis inhibitor.

ecMetAP-IN-1 can be used as a QSAR model to study methionine aminopeptidase inhibitor as an anticancer agent using multiple linear regression.

Sar-[D-Phe8]-des-Arg9-Bradykinin acetate is a potent and selective bradykinin B1 receptor agonist (EC50 = 9.02 nM in rabbit aorta) that is resistant to aminopeptidase, kininase I and II (ACE) and neutral endopeptidase cleavage. Exhibits hypotensive and angiogenic activity in vivo.

ERAP1-IN-1 is an endoplasmic reticulum aminopeptidase 1 (ERAP1) inhibitor that allosterically activates ERAP1's hydrolysis of fluorogenic and chromogenic amino acid substrates, while competitively inhibiting its activity toward a nonamer peptide representative of physiological substrates.

TP-004 is a potent, reversible inhibitor of methionine aminopeptidase 2 (MetAP2) with an IC50 of 6 nM.

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].

Puromycin aminonucleoside (NSC 3056) is an aminonucleoside antibiotic and a purine analog of puromycin. It can reversibly inhibit dipeptidyl peptidase and cytosolic alanine aminopeptidase, increase podocyte permeability by regulating ZO-1 in an oxidative stress-dependent manner, induce apoptosis, and promote the secretion of migrasomes. It is commonly used to induce nephrotic syndrome models in research.

SB-587094 is a reversible inhibitor of methionine aminopeptidase-2 (MetAP-2).

ERAP1 modulator-1 (Compound 1) is a regulator of endoplasmic reticulum aminopeptidase 1 (ERAP1) with an IC50 of less than 250 nM.

ERAP1-IN-3 (compound 13) is a potent inhibitor of endoplasmic reticulum aminopeptidase 1 (ERAP1), with a pIC50 value of 8.6. ERAP1-IN-3 shows potential for research in cancer immunotherapy and autoimmune disease studies.

L-Leucine-p-nitroanilide is a substrate. It is used for the colorimetric determination of leucine aminopeptidase.

Apstatin TFA is a potent inhibitor of aminopeptidase P (APP), with Ki values of 2.6 µM for rat APP and 0.64 µM for human APP. This compound also exhibits cardioprotective properties.

L-Val-P is an effective inhibitor of leucine aminopeptidase (LAP) with a Ki value of 0.15 μM. It holds significant potential for research in HIV infection, inflammation, cataracts, and cancer.

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.

Amastatin is a non-toxic inhibitor of aminopeptidase A and leucine aminopeptidase, and its Ki for aminopeptidase A is 1 µM .

Matlystatin A is an inhibitor of aminopeptidase. It shows multiple inhibitory activities against both aminopeptidase N and matrix metalloproteinases.

Ketomethylenebestatin is a carba-analog of bestatin,the aminopeptidase (AP) inhibitor. Ketomethylenebestatin is 10 fold less effective as an inhibitor of aminopeptidases than bestatin.

Microginin 527, a compound found in Microcystis, is an inhibitor of protein phosphatase, ACE, and leucine aminopeptidase.

7-Lysylalanyl-4-methylcoumarinamide is a Fluorogenic substrate for dipeptidyl aminopeptidase.

Leucylmethionine is a substrate for aminopeptidase M.

Tripeptidyl peptidase II (TPPII) is a serine peptidase of the subtilisin-type which removes tripeptides from the free NH2 terminus of oligopeptides. AAF-CMK is an irreversible inhibitor of TPPII commonly used at 10-100 μM. It does not significantly interfere with the chymotrypsin-like activity of the proteasome. AAF-CMK also inhibits bleomycin hydrolase and puromycin-sensitive aminopeptidase when used at 50 μM.