synthetase

CTP Synthetase-IN-1 Ammonium salt is an orally active and potent cytidine 5'-triphosphate synthetase (CTPS) inhibitor with potential antimicrobial, anti-inflammatory and antitumor activity for the study of SARS-CoV-2 viral infections.

CTP Synthetase-IN-1 is an orally active and potent cytidine 5'-triphosphate synthetase (CTPS) inhibitor with potential antitumour activity, shows anti-inflammatory activity in animal models of inflammation, inhibits human CTPS1 and human CTPS2, and can be used in studies of arthritis and rheumatoid arthritis.

Aminoacyl tRNA synthetase-IN-1 is an inhibitor of bacterial aminoacyl tRNA synthetase (aaRS).

Trypanothione Synthetase-IN-1 (Compound 1) serves as a competitive inhibitor of Leishmania infantum trypanothione synthetase (TryS), demonstrating an IC50 value of 14.8 μM in the presence of the polyamine S, triamine spermidine [1].

NAD Synthetase is responsible for the final step in the synthesis of Nicotinamide Adenine Dinucleotide (NAD). The enzyme sourced from Escherichia coli exhibits Km values of 200 μM for NAD, 11 μM for ATP, and 0.65 μM for ammonia. Conversely, NAD Synthetase derived from yeast demonstrates Km values of 170 μM for NAD, 190 μM for ATP, and 64 μM for ammonia. This enzyme is applicable in enzymatic assays for ATP, ammonia, urea, or creatinine and can also be used in enzymatic recycling methods. Additionally, NAD Synthetase holds potential for research into metabolic diseases, cancer, aging, and neurodegenerative disorders.

Trypanothione Synthetase-IN-2 (Compound 3) functions as a competitive inhibitor of Leishmania infantum trypanothione synthetase (TryS), demonstrating an inhibition constant (IC50) of 5.4 μM in the presence of the polyamine S, triamine spermidine [1].

Isoleucyl tRNA synthetase-IN-1 is a selective and potent inhibitor (Ki: 88 nM) that targets isoleucyl tRNA synthetase (IleRS).

Isoleucyl tRNA synthetase-IN-2 is a selective and potent inhibitor (Ki: 114 nM) that targets isoleucyl tRNA synthetase (IleRS).

Trypanothione Synthetase-IN-3, a mixed noncompetitive inhibitor of Trypanothione Synthetase (TryS) with an inhibition constant (Ki) of 0.8 μM, is useful in researching parasites like L. infantum [1].

Acyl coenzyme A synthetase (ACS), also known as acetyl coenzyme A synthetase, catalyzes the activation of fatty acids via coenzyme A through a two-step thioesterification process, forming acyl coenzyme A. It is crucial in anabolic and catabolic lipid metabolism pathways and contributes to the tricarboxylic acid (TCA) cycle during aerobic respiration [1].

Trypanothione synthetase-IN-4, a L. infantumTryS inhibitor, exhibits a strong anti-leishmanicidal effect (EC50: 0.6 μM, SI) dependent on the concentration of the polyamine substrate and can be used to study leishmaniasis.

Aminoacyl tRNA Synthetase-IN-2 (Compound 14) serves as an inhibitor of aminoacyl-tRNA synthetase (aaRS), presenting potential for the formulation of a novel class of antibiotics [1].

Bersiporocin is a novel prolyl-tRNA synthetase (PRS) inhibitor that exerts antifibrotic effects through downregulation of collagen synthesis and is well tolerated in the clinic. In cellular and animal models of idiopathic pulmonary fibrosis (IPF), DWN12088 significantly reduced collagen synthesis and improved lung function.

CGS 15435 is a potent thromboxen (TxA2) synthetase inhibitor (IC50: 1 nM). CGS 15435 acts on PGI2 synthase, cyclooxygenase and liposynthase with much less selectivity than on thromboxin synthase.

Pirodomast is a thromboxane A (TXA2) synthase inhibitor. Pirodomast inhibits leukotriene (LT) D4, C4, E4 formation and thromboxane B2 (TXB2) activity, but is weakly or ineffectively antagonistic to guinea pig bronchospasm induced by histamine, methacholine, serotonin, LTC4, or platelet-activating factor. Pirodomast is a potential antiallergic compound. Pirodomast had only weak relaxant activity on guinea pig trachea in vitro. Pirodomast is a potential antiallergic compound that inhibits the protein hydrolyzing activity of trypsin in vitro, prevents antigen-induced immediate and late asthmatic responses in allergic sheep in vivo, and inhibits antigen-induced airway hyperresponsiveness to histamine and carbachol in allergic sheep.

LeuRS-IN-1 is an orally active and potent Mycobacterium tuberculosis leucyl-tRNA synthetase inhibitor with anti-leukemic and anti-malarial activity, inhibits M.tb LeuRS, inhibits HepG2 protein synthesis, and can be used in leukemia research.

D75-4590 is a β-1,6-Glucan inhibitor. As glucan is a major component of the cell wall, specifically β-1,6-Glucan, D75-4590 can fight fungal infections by inhibiting its synthetase.

Sinbaglustat (OGT2378) (OGT2378) is a dual inhibitor of glucose ceramide synthetase (GCS) and non-lysosomal glucose ceramidase (GBA2).Sinbaglustat is an orally administered N-alkyl iminosugar that crosses the blood-brain barrier.Sinbaglustat is used for the treatment of lysosomal storage disorders and for the study of central neurodegenerative disorders associated with lysosomal dysfunction. Sinbaglustat is used for the treatment of lysosomal storage disorders and for the study of lysosomal dysfunction-related central neurodegenerative diseases.

SMS2-IN-1 is an effective and highly selective sphingomyelin synthetase 2 (SMS2) inhibitor with IC50 of 6.5 nM and Kd of 37 nM. Sms2-in-1 is 150 times more selective to SMS2 than SMS1 (IC50 is 1000 nM).

RS-601 is a potent dual leukotriene D4 thromboxane A2 inhibitor that inhibits antigen-induced airway hyperresponsiveness (AHR) and shows asthmatic effects in a guinea pig model of asthma.

Imitrodast is a small molecule thromboxane A2 synthase (TXA2 synthase) inhibitor for the treatment of immune system disorders, respiratory disorders, and cardiovascular diseases, and can be used in studies of arterial thrombosis, asthma, and coronary vasospasm.

LysRs-IN-1 is an inhibitor of Lysyl-tRNA synthetase (LysRs).

Ozagrel (Domenan) is a selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.

4-Methylsalicylic acid is used to inhibit the medium chain acyl-CoA synthetase.