synthetase

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).

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.

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].

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

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-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, plays a pivotal role in biochemical research. This enzyme catalyzes the activation of fatty acids via coenzyme A through a two-step thioesterification process, resulting in the formation of acyl coenzyme A. Subsequently, it is involved in numerous anabolic and catabolic lipid metabolism pathways and contributes to the tricarboxylic acid (TCA) cycle during aerobic respiration [1].

Trypanothione synthetase-IN-4 is a L. infantumTryS inhibitor whose activity is dependent on the concentration of the polyamine substrate. trypanothione synthetase-IN-4 exhibits a strong anti-leishmanicidal effect (EC50: 0.6 μM, SI ( Trypanothione synthetase-IN-4 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].

VY-3-135 is a metastasis inhibitor and an acetyl-CoA synthetase 2 (ACSS2) modulator.

Phenylmethanesulfonyl fluoride (PMSF (Phenylmethylsulfonyl fluoride)) is an enzyme inhibitor that inactivates IRC-50 arvin, subtilisin, and the fatty acid synthetase complex.

L-Asparagine (Asparamide) is a non-essential amino acid that is involved in the metabolic control of cell functions in nerve and brain tissue. It is biosynthesized from ASPARTIC ACID and AMMONIA by asparagine synthetase.

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.

HALOFUGINONE LACTATE is a halogenated derivative of febrifugine, a natural quinazolinone-containing compound found in the Chinese herb D. febrifuga.Halofuginone inhibits prolyl-tRNA synthetase in an ATP-dependent manner with a Ki of 18.3 nM. Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity

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.

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).

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

Halofuginone specifically inhibits collagen type I gene expression and matrix metalloproteinase 2 (MMP-2) gene expression, which may result in the suppression of angiogenesis, tumor stromal cell development, and tumor cell growth. Halofuginone Hydrobromide is the hydrobromide salt of halofuginone, a semisynthetic quinazolinone alkaloid anticoccidial derived from the plant Dichroa febrifuga, with antifibrotic and potential antineoplastic activities. These effects appear to be due to halofuginone-mediated inhibition of the collagen type I and MMP-2 promoters. Collagen type I and MMP-2 play important roles in fibroproliferative diseases.

5-Hydroxydecanoate sodium is a selective ATP-sensitive K+ (KATP) channel blocker with IC50 of about 30 μM. 5-Hydroxydecanoate sodium is a substrate for mitochondrial outer membrane acyl-CoA synthetase with antioxidant property.

Aspirin (Acetylsalicylic Acid) is a potent and selective inhibitor of COX with various pharmacological activities, such as anti-inflammation and pain relief. Aspirin is a histone deacetylase inhibitors to up-regulate cell cycle arrest protein p21, which can suppresses ovarian Y cells harboring COX-1. Aspirin also inhibits the expression of COX-2 in HUVEC and neonatal rat ventricular cardiomyocytes, and then reduce PG production and the down-regulation of ERK and NF-KB, respectively.

PRGL493 is an inhibitor of long-chain acyl-CoA synthetase 4 (ACSL4).1It inhibits formation of arachidonoyl-CoA (AA-CoA) from arachidonic acid in, as well as the proliferation and migration of, PC3 and MDA-MB-231 cancer cells when used at a concentration of 50 μM. PRGL493 (5 μM) reduces production of progesterone induced by 8-Br-cyclic AMP (8-Br-cAMP) in MA-10 Leydig tumor cells. It inhibits tumor growth in a PC3 mouse xenograft model when administered at a dose of 0.25 mg/kg.

5-Fluorouracil-13C,15N2 is intended for use as an internal standard for the quantification of 5-flurouracil by GC- or LC-MS. 5-Fluorouracil is a pyrimidine analog that irreversibly inhibits thymidylate synthase, blocking the synthesis of thymidine which is required for DNA synthesis. Intracellular metabolites of 5-fluorouracil exert cytotoxic effects by either inhibiting thymidylate synthetase, or through incorporation into RNA and DNA, ultimately initiating apoptosis.

Omega-3 Arachidonic Acid ethyl ester, a rare polyunsaturated fatty acid with limited presence in dietary sources, is crucial for infant growth and development and offers protection against heart disease, blood clots, high blood pressure, and inflammatory and autoimmune disorders. In human platelet membranes, it impedes arachidonyl-CoA synthetase, exhibiting a Ki of 14 μM, and shows similar inhibitory effects on arachidonoyl-CoA synthetase in calf brain extract with an IC50 of roughly 5 μM. The ethyl arachidonate derivative offers enhanced lipophilicity compared to its free acid counterpart.

AGI-24512 is a potent inhibitor of methionine adenylyltransferase 2α (MAT2A) (IC50: 8 nM).AGI-24512 shows antiproliferative activity in MTAP-deficient cancer cells.AGI-24512 inhibits MAT2A, which causes DNA damage in MTAP, and is often used in conjunction with anticancer compounds in cancer research.

Ozagrel hydrochloride (OKY-046 HCl) is a selective thromboxane A(2) synthetase inhibitor used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.

LeuRS-IN-1 hydrochloride is a potent and orally active inhibitor of M. tuberculosis leucyl-tRNA synthetase (M.tb LeuRS). It has IC 50 and Kd values of 0.06 μM and 0.075 μM, respectively, for M.tb LeuRS. Additionally, LeuRS-IN-1 hydrochloride inhibits human cytoplasmic LeuRS with an IC 50 of 38.8 μM and HepG2 protein synthesis with an EC 50 of 19.6 μM.

PGS-IN-1 (KME-4) is a potent inhibitor of prostaglandin synthetase (PGS, IC50: 0.28 μM) and 5-lipoxygenase (IC50: 1.05 μM).

Thioacetamide-S-oxide, a metabolite of Thiocetamide, functions as a δ-aminolevulinic acid (ALA) synthetase inhibitor [1].

Cryogenine is an alkaloid originally isolated from H. salicifolia that has anti-inflammatory activity.1 It inhibits prostaglandin synthetase (IC50 = 424 μM). Cryogenine (100 mg/kg per day, p.o.) reduces paw edema and the mean arthritic index in a rat model of adjuvant-induced polyarthritis.2 |1. Lema, W.J., Blankenship, J.W., and Malone, M.H. Prostaglandin synthetase inhibition by alkaloids of Heimia salicifolia. J. Ethnopharmacol. 15(2), 161-167 (1986).|2. Kosersky, D.S., Brown, J.K., and Malone, M.H. Effects of cryogenine on adjuvant-induced arthritis and serum turbidity in rats. J. Pharm. Sci. 62(12), 1965-1971 (1973).

3-Deazauridine (NSC-126849) is a structural analog of uridine that inhibits the biosynthesis of Cytidine-5'-Triphosphate by competitive inhibition of Cytidine Triphosphate synthetase which is considered to be the primary mode of action of this nucleoside analog.

SB-217452 is a potent seryl tRNA synthetase inhibitor isolated from Streptomyces.

2-Hydroxyoctanoic acid is a medium-chain acyl-coenzyme A synthetase inhibitor (Ki:500 μM). 3-Hydroxymandelic acid is a protein hydrolysis product of larger proteins.

N-Formyl-L-histidine demonstrates a binding affinity for histidyl-tRNA synthetase, featuring a K i value of 4.6 μM. Additionally, it acts as a competitive inhibitor against L-histidine ammonia-lyase, suppressing urocanic acid formation from L-histidine with a K i value of 4.26 mM [1] [2].

10-Formyldihydrofolate is a Methotrexate metabolite. It inhibits thymidylate synthetase and glycinamide ribotide transformylase.

FPL 62064 is a potent dual inhibitor of 5-lipoxygenase (5-LOX) and COX (IC50 of 3.5 μM and 3.1 μM for RBL-1 cytosolic 5-lipoxygenase and prostaglandin synthetase, respectively).

Aureusimine B, also known as phevalin, is a natural pyrazinone produced by certain fungi and by Staphylococcus spp., including S. aureus. Its synthesis appears to be initiated by a conserved nonribosomal peptide synthetase that creates a dipeptide (phenylalanine-valine) aldehyde, which then undergoes cyclization and oxidation. Aureusimine B inhibits calpain in a casein hydrolysis assay (IC50 = 1.3 μM), contributes to S. aureus infection in mice, and alters human keratinocyte gene expression.

Polyoxin D (Polyoxorim), a polyoxin antibiotic fungicide, effectively inhibits chitin synthetase.

LeuRS-IN-1 is a highly potent and orally active inhibitor of the leucyl-tRNA synthetase enzyme derived from Mycobacterium tuberculosis (M.tb LeuRS). It exhibits significant inhibitory activity against M.tb LeuRS with IC 50 and Kd values of 0.06 μM and 0.075 μM, respectively. Additionally, LeuRS-IN-1 effectively inhibits human cytoplasmic LeuRS with an IC 50 value of 38.8 μM and suppresses protein synthesis in HepG2 cells with an EC 50 value of 19.6 μM.

L-Methioninamide hydrochloride is a potent inhibitor of methionyl-tRNA synthetase that reduces the toxicity of CDDP.

Borrelidin (Treponemycin) is a bacterial and eukaryal threonyl-tRNA synthetase inhibitor. It is a macrolide antibiotic isolated from Streptomyces rochei.

Dihydrohomofolic acid is a substrate for dihydrofolate reductase that produces tetrahydro-homo folate which in turn suppresses thymidylate synthetase and then DNA synthesis.

CRS3123 (REP-3123) dihydrochloride is an orally active, fully synthetic antimicrobial agent that effectively inhibits Clostridioides difficile methionyl-tRNA synthetase (MetRS). CRS3123 dihydrochloride can be used in the study of Clostridioides difficile infection (CDI).

Asp-AMS is a strong competitive inhibitor of the mitochondrial enzyme and also an aspartyl-tRNA synthetase inhibitor.

ThrRS-IN-1 (Compound 30d) is a potent inhibitor of threonyl-tRNA synthetase (ThrRS) from Salmonella enterica (Se ThrRS), exhibiting an IC50 of 1.4 μM and a Kd of 1.36 μM. It uniquely targets both the tRNA Thr and L-threonine binding sites of ThrRS, demonstrating significant antibacterial activities [1].

Antibacterial agent 92, a triple-site aminoacyl-tRNA synthetase (aaRS) inhibitor, demonstrates a potent antibacterial effect by inhibiting Salmonella enterica threonyl-tRNA synthetase (SeThrRS) with an IC50 of 0.58 μM.

T-3861174 is a prolyl tRNA synthetase (PRS) inhibitor, exhibiting significant in vitro anti-tumor activity with GCN2-ATF4 pathway activation.

DL-Buthionine-(S,R)-sulfoximine hydrochloride (Buthionine sulfoximine hydrochloride) is a potent and specific glutamylcysteine synthetase biosynthesis inhibitor.

DS86760016 is a highly effective inhibitor of leucyl-tRNA synthetase (LeuRS), demonstrating potent activity against multidrug-resistant (MDR) Gram-negative bacteria including Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa. Notably, DS86760016 effectively inhibits LeuRS enzymes derived from Escherichia coli, Pseudomonas aeruginosa, and Acinetobacter baumannii, exhibiting IC50 values of 0.38 μM, 0.62 μM, and 0.16 μM, respectively.