aldolase

Aldometanib (LXY-05-029) is an orally active aldolase inhibitor that prevents FBP from binding to v-ATPase-associated aldolase and activates lysosomal AMPK, useful in metabolic homeostasis research [1].

Aldolase is a glycolytic enzyme and component of the VATPase complex that catalyzes the reversible cleavage of fructose 1,6-bisphosphate into dihydroxyacetone phosphate and D-glyceraldehyde 3-phosphate. Aldolase plays a critical role in cellular energy metabolism, metabolic flux regulation, and enzymatic studies of glycolysis and related pathways.

Sialic acid aldolase (Pm NaNa) (EC 4.1.3.3) is a type I aldolase that catalyzes the reversible aldol cleavage of N-acetylneuraminic acid (Neu5Ac) to produce pyruvate and N-acetyl-D-mannosamine (ManNAc), with the equilibrium favoring the cleavage of Neu5Ac.

Aldolase, Spinach (EC 4.1.2.13), is an enzyme that catalyzes a reversible reaction in which aldol (fructose-1,6-bisphosphate) is cleaved into three-phosphate glyceraldehyde (dihydroxyacetone phosphate, DHAP) and glyceraldehyde-3-phosphate (G3P). It can also utilize other (3S,4R)-ketose-1-phosphates, such as fructose-1-phosphate and sedoheptulose-1,7-bisphosphate, to produce DHAP.

3-Deoxy-D-manno-octulosonate Aldolase, E.coli (EC 4.1.2.23) is an enzyme in the aldolases family that catalyzes the cleavage of carbon-carbon bonds. This enzyme acts on the substrate 3-deoxy-D-manno-octulosonate, producing two products: pyruvate and D-arabinose.

Aldolase A, Human (EC 4.1.2.13), is a glycolytic enzyme that catalyzes the reversible conversion of fructose-1,6-bisphosphate into glyceraldehyde-3-phosphate and dihydroxyacetone phosphate. It is expressed in Escherichia coli with an N-terminal His tag.

(4S)-4-Hydroxy-2-oxoglutarate aldolase (EC 4.1.3.42) is specific to the (S) enantiomer. It catalyzes the reactions of oxaloacetate decarboxylase (EC 4.1.1.3) and 2-dehydro-3-deoxyphosphogluconate aldolase (EC 4.1.2.14).

Transaldolase, from Baker's yeast (S. cerevisiae) (EC 2.2.1.2), is an enzyme involved in the non-oxidative phase of the pentose phosphate pathway. It catalyzes the conversion of sedoheptulose 7-phosphate and glyceraldehyde 3-phosphate into erythrose 4-phosphate and fructose 6-phosphate.

Metronidazole (Metronidazol) is a synthetic nitroimidazole derivative with antiprotozoal and antibacterial activities.

TLK117 is an inhibitor of GSTs that reduces the severity of pulmonary fibrosis and can be used to study idiopathic pulmonary fibrosis.

ALDOA-IN-1 is an inhibitor of aldolase A (ALDOA). It directly suppresses ALDOA enzyme activity, leading to reduced lactate production, downregulation of HIF-1α expression, and ultimately inducing apoptosis in cancer cells. ALDOA-IN-1 is applicable for colorectal cancer research.

FBA-IN-1 (compound 2a11) is a first-in-class, covalent, and allosteric inhibitor of fructose-1,6-bisphosphate aldolase (FBA) from Candida albicans (CaFBA). Additionally, FBA-IN-1 inhibits the growth of Azole-resistant strains 103 with an MIC 80 of 1 μg/mL [1].

Piperazine (2HCl) is gamma-aminobutyric acid (GABA) agonists and its major effects appear to be on the central nervous system. Piperazine was the anthelmintic with the greatest number of reports of toxicoses and suspected toxicoses in cats. Piperazine neurotoxicity in cats and dogs usually was manifested by muscle tremors, ataxia, and/or behavioral disturbances within 24 hours after estimated daily dose(s) between 20 and 110 mg/kg[1]. For di-substituted derivatives, ciprofloxacin was selected and hybrids were synthesized via substitution at piperazinyl-N4. The reaction of piperazinyl-NH of ciprofloxacin with selected drugs resulted in pronounced growth inhibition of standard as well as resistant bacterial strains[2]. The parent piperazine 6 was found to exhibit a reasonable activity toward the HeLa and MDA MB 231 tumor cell lines (IC50= 9.2 and 8.4 μΜ, respectively)[3]. Piperazine adipate (10 mM) causes mortality of A. galli and H. gallinae after a maximum of 30 min exposure, inhibits malate oxidation by 78%, and inhibits aldolase activity in both parasites. Piperazine adipate (10 mM) also inhibits cholinesterase activity by 96% in Ascaridia galli (A. galli) and 93% in Heterakis gallinae (H. gallinae). Piperazine adipate inhibits oxaloacetate reduction by 26% and 55% in A. galli and H. gallinae, resepctively[4].

KRH102053 is a HIF-1alpha inhibitor. KRH102053 decreased the protein level of HIF-1alpha and the mRNA levels of HIF-regulated downstream target genes, such as vascular endothelial growth factor, aldolase A, enolase 1 and monocarboxylate transporter 4. Consistent with these results, KRH102053 also inhibited the rates of HIF-related migration and invasion of HOS cells as well as the degree of tube formation in human umbilical vein endothelium cells.

Phosphoglycolohydroxamic acid, acting as a potent inhibitor of both aldolase and triose-phosphate isomerase, serves a crucial role in the research of antibacterial and antifungal domains.

N-Acetylneuraminate lyase (CgNal) (Sialic acid aldolase (CgNal)), a class I aldolase frequently utilized in biochemical research, catalyzes the reversible condensation of pyruvate and N-acetyl-d-mannosamine (ManNAc), producing N-acetylneuraminic acid (Neu5Ac) [1].

2-Deoxyribose 5-phosphate disodium acts as a substrate for the enzyme 2-deoxyribose-5-phosphate aldolase (DERA), which is categorized under class I aldolases. DERA efficiently facilitates the reversible aldol condensation reaction independently, without the need for any cofactors [1].

2-Keto-3-deoxy-6-phosphogluconate is an endogenous metabolite found in E. coli and serves as a crucial intermediate in both the Entner-Doudoroff (ED) pathway and the breakdown pathways of gluconates and sugar polymers in human and plant pathogens, produced by the catalytic action of KDPG aldolase.

DL-4-Hydroxy-2-ketoglutarate lithium is a substrate for 4-hydroxy-2-oxoglutarate aldolase (HOGA), which can be cleaved by HOGA into pyruvate and glyoxylate.

DL-4-Hydroxy-2-ketoglutarate (DL-4KG) is a gamma-keto acid as well as a structural analogue of glutamic acid that functions as a biochemical substrate for enzymes such as 4-hydroxy-2-oxoglutarate aldolase (HOGA1) and glutamic-oxaloacetic transaminase (GOT),DL-4-Hydroxy-2-ketoglutarate also serves as a lysine analogue used in mechanistic studies of enzyme inhibition and metabolic pathways.