Arginase

Numidargistat dihydrochloride (CB-1158 dihydrochloride) is an orally active and highly effective arginase (ARG1) inhibitor, an immuno-oncology agent that inhibits TGF-β2-induced subcapsular cataract by reducing the proliferation of lens epithelial cells (LEC) and decreasing the expression of fibronectin, α-SMA, collagen 1A1, and vimentin.

L-Ornithine ((S)-2, 5-diaminopentanoic acid) is a non-protein amino acid. L-Ornithine is mainly used in the urea cycle to remove excess nitrogen from the body. L-Ornithine is renoprotective. L-Ornithine has antifatigue effects.

BEC hydrochloride (BEC HCl) is a competitive arginase inhibitor, which bind slowly. Ki of BEC HCl is 0.31 μM (pH7.5) for Arginase II, and is 0.4-0.6 μM for rat Arginase I.

Nω-Hydroxy-nor-L-Arginine Dihydrochloride is a competitive and reversible inhibitor of arginase

Urea (Carbonyldiamide) is formed in the liver from ammonia produced by the deamination of amino acids. It is the principal end metabolite of protein catabolism and accounts for about one-half of the total urinary solids.

Piceatannol 3'-O-glucoside (Piceatannol 3-glycoside) increases pulmonary blood oxygen tension and decreases pulmonary interstitial edema, so it can protect lung injury.

Guanidine hydrochloride (Aminoformamidine Hydrochloride) is a strong organic base existing primarily as guanidium ions at physiological pH. It is found in the urine as a normal product of protein metabolism. It is also used in laboratory research as a protein denaturant.

L-Norvaline is an arginase inhibitor and a non-protein branched-chain amino acid. L-Norvaline has previously been reported as a natural component of the antifungal peptide of Bacillus subtilis. L-Norvaline and other modified branched-chain amino acids have received attention in recent studies because they appear to be incorporated into some recombinant proteins found in E. coli.

DL-Norvaline (2-Aminopentanoic acid) is a non-competitive inhibitor of arginase.

2-Aminoimidazole is a potent antimicrobial agent that effectively targets drug-resistant Mycobacterium tuberculosis by disrupting the proton motive force and blocking the electron transport chain, potentiates the action of beta-lactam antibiotics against Mycobacterium tuberculosis by decreasing the secretion of beta-lactamases and increasing the permeability of cell membranes, activates drug-resistant bacteria and improves therapeutic efficacy.

nor-NOHA monoacetate (Nω-Hydroxy-nor-L-arginine) is a highly potent and selective arginase inhibitor. nor-NOHA monoacetate inhibits rat hepatic arginase and inhibits the hydrolysis of L-arginine, which can be used to study cardiovascular and obstructive airway diseases.

nor-NOHA acetate (Nω-Hydroxy-nor-L-arginine acetate) is a reversible inhibitor of arginase with anti-leukemic activity, effective in treating endothelial dysfunction, immunosuppression, and metabolism regulation.

NED-3238 is a highly potent inhibitor of arginase I and II (IC50: 1.3 nM and 8.1 nM, respectively).

Arginase Inhibitor 7 (compound A17), an inhibitor of arginase (ARG1), exhibits an IC 50 value of 0.16 μM and possesses high oral bioavailability [1].

OATD-02 is an orally active, competitive, reversible, noncovalent inhibitor with slow offset kinetics that targets both Arginase1 and Arginase2, exhibiting inhibitory concentrations (IC50) of 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), and 28 nM (rARG1). Notably, OATD-02 mitigates tumor immunosuppression provoked by these arginases and has potential application in melanoma research [1].

Arginase inhibitor9 (Compound 12a) is a type of arginase enzyme inhibitor with IC50 values of 9 μM for bovine and 55 μM for human arginase I. It also exhibits antioxidant activity by scavenging free radicals. Moreover, Arginase inhibitor9 effectively regulates collagen and procollagen levels, thereby exerting an anti-fibrotic effect.

ARG1-IN-1 hydrochloride is a potent inhibitor of human arginase 1, exhibiting an IC50 value of 29 nM [1].

NG-Hydroxy-L-arginine acetate (NOHA acetate) acts as a crucial physiological inhibitor of arginase, playing a vital role in the conversion of arginine to nitric oxide and citrulline via nitric oxide synthase.

Broussonin E could suppress inflammation by modulating macrophages activation state via inhibiting the ERK and p38 MAPK and enhancing JAK2-STAT3 signaling pathway, and can be further developed as a promising drug for the treatment of inflammation-related

CB-1158 is a potent and orally bioavailable inhibitor of arginase (IC50s: 86 and 296 nM for recombinant human arginase 1 and 2).

ARG1-IN-1 is a human arginase 1 inhibitor with an IC 50 of 29 nM.

ABH Hydrochloride is an arginase inhibitor, it enhances both male and female sexual arousal responses.

OATD-02 hydrochloride is the hydrochloride salt form of OATD-02. It is an orally effective, competitive, reversible, and non-covalent dual inhibitor of Arginase1 and Arginase2. OATD-02 hydrochloride serves as a sustained-release inhibitor that efficiently blocks the activity of intracellular arginases, with IC50 values of 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), and 28 nM (rARG1). It effectively eliminates tumor-induced immunosuppression caused by both types of arginases. This compound is utilized in research studies on melanoma.

Arginase inhibitor 1 is a potent inhibitor of human arginases I and II [IC50s: 223 and 509 nM].