lyase

Cystathionine-γ-lyase-IN-1 (SHIP-2a) is a selective inhibitor of cystathionine γ-lyase (CSE) enzyme (IC50= 6.3 μM).

L-Methionine γ-lyase (Methionine lyase), a multifaceted enzyme in the γ-family of pyridoxal-5’-phosphate (PLP)-dependent enzymes, catalyzes the α, γ-elimination of L-methionine and homocysteine. This enzyme exhibits anticancer and anti-infectious properties and is utilized in homocysteinemia research [1] [2] [3].

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].

Cystathionine β-lyase, an enzyme crucial for bacterial virulence [1], catalyzes the conversion of cystathionine into homocysteine, representing the penultimate step in the biosynthesis of methionine.

Pectate Lyase, an enzyme secreted by plant pathogens, is essential for pectin degradation and plays a vital role in fungal virulence. Additionally, it triggers plant immune responses, further contributing to its virulence [1].

S1PL-IN-31 is a dual-function chemical compound acting as an inhibitor of sphingosine-1-phosphate (S1P) lyase with an IC50 value of 210 nM and as an antagonist of the Smoothened (Smo) receptor with an IC50 of 440 nM. Demonstrating therapeutic potential, this compound, at a dosage of 2 mg/kg per day, effectively mitigates cervical and thoracic lymphocyte infiltration and neuromuscular weakness in rats suffering from experimental autoimmune encephalomyelitis (EAE), a condition triggered by the MOG29-152 peptide from myelin oligodendrocyte glycoprotein. Additionally, it significantly decreases the total lymphocyte count, including reductions in subsets of CD4+ T cells, CD8+ T cells, and B cells. At a higher dosage of 100 mg/kg, S1PL-IN-31 elevates S1P levels within the heart and lymph nodes, while doses of 3 and 10 mg/kg per day notably lower heart rates in female rats, showcasing its multifaceted biological impacts and potential for clinical application.

SB 204990 is an effective and specific ATP citrate lyase enzyme inhibitor.

Hydroxycitric acid tripotassium hydrate (Potassium citrate monohydrate) effectively inhibits stones formation and also inhibits HIF, and has antioxidation, anti-inflammation, and anti-tumor effects. Hydroxycitric acid tripotassium hydrate(Potassium citrate monohydrate) (Potassium citrate monohydrate) is the major active ingredient of Garcinia cambogia and a derivative of citric acid. Hydroxycitric acid tripotassium hydrate(Potassium citrate monohydrate) competitively inhibits ATP citrate lyase with weight loss benefits.

2-Furoic acid (Furan-2-carboxylic acid) 2-Furoic acid can reduce serum cholesterol and triglyceride levels and has anti-lipidemic effects.

L-Cysteine S-sulfate (S-Sulfo-L-cysteine) is an effective N-methyl-d-aspartate (NMDA) glutamatergic receptors agonist. L-Cysteine S-sulfate is the substrate for cystine lyase [1].

2-Propen-1-one, 1-(2,6-dimethoxyphenyl)-3-(4-hydroxyphenyl)- can be used in studies about the inhibition against L-phenylalanine ammonia-lyase.

MEDICA16 is a selective agonist for GPR40 as well as a partial agonist for GPR120. MEDICA16, an ATP-citrate lyase inhibitor, significantly reduces intracellular TG content in gastrocnemius muscle with an increase in insulin sensitivity.

Galeterone (VN 124) is an orally bioavailable small-molecule androgen receptor modulator and CYP17 lyase inhibitor with potential antiandrogen activity. Galeterone exhibits three distinct mechanisms of action: 1) as an androgen receptor antagonist, 2) as a CYP17 lyase inhibitor and 3) by decreasing overall androgen receptor levels in prostate cancer tumors, all of which may result in a decrease in androgen-dependent growth signaling. Localized to the endoplasmic reticulum (ER), the cytochrome P450 enzyme CYP17 (P450C17 or CYP17A1) exhibits both 17alpha-hydroxylase and 17, 20-lyase activities, and plays a key role in the steroidogenic pathway that produces progestins, mineralocorticoids, glucocorticoids, androgens, and estrogens.

BMS-303141 is a potent ATP-citrate lyase (ACL) inhibitor (IC50: 0.13 uM, human recombinant ACL).

Abiraterone (CB-7598) (CB-7598) is an effective steroidal cytochrome P450 17alpha-hydroxylase-17, 20-lyase (CYP17) inhibitor (IC50: 4 nM).

Methylglutaric acid is a leucine metabolite. A large amount of methylglutaric acid is identified in urine of patients with deficiency of 3-methylglutaconyl coenzyme A hydratase (PMID 6181239 ). Methylglutaric acid is also found to be associated with 3-hyd

Antimycin A4 is an active component of the antimycin A antibiotic complex that is more polar than antimycin A1 , antimycin A2 , and antimycin A3 . Antimycin A4 inhibits ATP-citrate lyase with a Ki value of 64.8 μM. The antimycin A complex is a mixture of antimycins A1, A2, A3, and A4 that demonstrates antifungal, insecticidal, nematocidal, and piscicidal properties. It blocks mitochondrial respiration and can deplete cellular levels of ATP via inhibition of complex III of the mitochondrial electron transport chain (ETC). Antimycin A prevents the transfer of electrons between the b-cytochromes and ubiquinone at the Q(inner) site of complex III. This results in the stabilization of the ubisemiquinone radical at the Q(outer) site of complex III, leading to increased production of superoxide. Antimycin A is widely used in research to shunt electron flow through the ETC to study the chemical details of oxygen respiration. Additionally, antimycin A has been shown to inhibit Bcl-2 and Bcl-xL proteins, inducing apoptosis.

Traumatic Acid (Dodec-2-Enedioic Acid) is a product of the hydroperoxide lyase pathway in plants. Potential as a wound healing agent that stimulates cell division near a wound site to form a protective callus.

TAK-700 salt is a potent and highly selective inhibitor of human 17,20-lyase with an IC50 of 38 nM and is over 1000-fold more selective than other CYPs such as 11-hydroxylase and CYP3A4.

Argininosuccinic acid disodium, involved in the urea cycle's fourth step, is cleaved by argininosuccinate lyase (ASL) into arginine and fumarate. It diminishes reduced glutathione (GSH) levels and elevates reactive oxygen species in the cerebral cortex and striatum, leading to lipid peroxidation, protein oxidation, and oxidative stress in the developing rat brain [1] [2].

DL-threo-2-methylisocitrate is a substrate of isocitrate lyase 1 (ICL1). Using Michaelis-Menten nonlinear least squares fitting, kcat value was 5.24 s-1, the Km of the purified recombinant ICL1 of threonine-D(s)L(s)-isocitrate (ICA) was 188 μM. The Km of

A6770 is an inhibitor of sphingosine-1-phosphate (S1P) lyase.1It induces accumulation of [3H]sphinganine-1-phosphate ([3H]dhS1P), an S1P lyase substrate, in IT-79MTNC3 cells that endogenously express high levels of S1P lyase (EC50= <0.01 μM), an effect that is reduced in the presence of vitamin B6(EC50= <100 μM). 1.Ohtoyo, M., Tamura, M., Machinaga, N., et al.Scintillation proximity assay to detect the changes in cellular dihydrosphingosine 1-phosphate levelsLipids51(10)1207-1216(2016)

L-2-Aminooxy-3-phenylpropanoic acid hydrobromide is a powerful inhibitor of L-phenylalanine ammonia-lyase, an enzyme responsible for catalyzing the conversion of L-phenylalanine to trans-cinnamic acid.

Acetoacetic acid, an endogenous metabolite found in cerebrospinal fluid and blood, is valuable for researching conditions such as meningitis, pregnancy, 3-hydroxy-3-methylglutaryl-CoA lyase deficiency, preeclampsia/eclampsia, Diabetes Mellitus Type 2, glucose transporter type 1 deficiency syndrome, and succinyl-CoA:3-oxoacid-CoA transferase deficiency [1] [2] [3] [4] [5] [6] [7].

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].

OGG1-IN-08 (OGG1-IN-O8) is an inhibitor of 8-oxoguanine DNA glycosylase 1 (OGG1;IC50 : 0.35 μM)

Gnetuhainin I (Compound 5), a lignin sourced from Pouzolzia zeylanica, exhibits potent inhibition of ATP citrate lyase (ACLY) with an IC50 value of 2.63 μM [1].

Adenylosuccinic acid (Adenylosuccinate; Aspartyl adenylate) is a purine ribonucleoside monophosphate and plays a role in nucleotide cycle metabolite. Adenylosuccinic acid has the potential for the study of duchenne muscular dystrophy(DMD)[1] and can be co

Seviteronel (VT-464) is a novel CYP17 cleavage enzyme inhibitor and androgen receptor antagonist for the study of breast and prostate cancer.

13(S)-HpOTrE is a monohydroperoxy polyunsaturated fatty acid produced in soybeans by the action of soybean LO-2 on esterified α-linolenic acid.[1] Incubation of soybean seedling biomembranes with soybean LO-2 catalyzes the formation of both 9- and 13-HpOTrE in a molar ratio of 10:1.1 In plants, 13(S)-HpOTrE can be metabolized by the hydroperoxide lyase pathway producing aldehyde and oxoacid fragments, or by the hydroperoxide dehydratase pathway producing jasmonic acid.[2],[3],[4] Treatment of tomato leaves with 13-HpOTrE causes induction of proteinase inhibitors, simulating the normal response to wounding.5 This data suggests that in plants 13(S)-HpOTrE may participate in a lipid-based signalling system initiated by insect and pathogen attack.

CFG920 is a CYP17 inhibitor, is also an orally available inhibitor of the steroid 17-alpha-hydroxylase/C17,20 lyase (CYP17A1 or CYP17), with potential antiandrogen and antineoplastic activities. Upon oral administration, CYP17 inhibitor CFG920 inhibits the enzymatic activity of CYP17A1 in both the testes and adrenal glands, thereby inhibiting androgen production. This may decrease androgen-dependent growth signaling and may inhibit cell proliferation of androgen-dependent tumor cells.

Edgeworin is a DNA polymerase beta (pol beta) inhibitor, it inhibits both the lyase and polymerase activities of DNA polymerase beta; it can potentiate the inhibitory action of the anticancer drug bleomycin in cultured A549 cells via an inhibition of DNA

SB-201076 is a potent ATP citrate-lyase inhibitor. SB-204990 is the prodrug of SB-201076.

Seviteronel R enantiomer is the R enantiomer of Seviteronel and is a potent inhibitor of CYP17 lyase (IC50: 69 nM for h-Lyase).

Liarozole dihydrochloride is a cytochrome P450 (CYP450) dependent inhibitor, orally active, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase).Liarozole dihydrochloride is an imidazole derivative; it is being investigated as a non-hormonal agent in prostate cancer and in the treatment of various other cancers and skin disorders.

Opevesostat (ODM-208) is an inhibitor of lyase (CYP11A1) (the enzyme cleavage cholesterol side chain).

TAK-700 (Orteronel) (Orteronel) is a potent and highly selective human 17, 20-lyase inhibitor with IC50 of 38 nM, exhibits >1000-fold selectivity over other CYPs (e.g. 11-hydroxylase and CYP3A4). Phase 3.

Citric acid trilithium salt tetrahydrate (Lithium citrate tribasic tetrahydrate) , the active component of Lithium, is a medicine used in the therapy of psychiatric disease. It has shown the effects of signaling pathways and metabolic in the brain based on the particular disease and clinical condition model. According to the reports, Citric acid trilithium salt tetrahydrate was used as a mood stabilizer when treating bipolar mood disorders (BD) and lower the risk of self-harm in BD patient. In addition,Citric acid trilithium salt tetrahydrate has been the choice drug in the therapy of acute manic episodes.Citric acid trilithium salt tetrahydrate also could dissolve uric acid crystals in urine achieved from patients with gout. Besides,Citric acid trilithium salt tetrahydrate have some dose-dependent side-effects. The the main side-effects of Lithium Citrate is the tendency to inhibit the prostatic acid phosphatase enzyme (PAP), which result in the accumulation of PAP.

Sphingosine-1-phosphate (S1P), a bioactive lipid crucial in numerous signaling pathways, undergoes irreversible degradation by membrane-bound S1P lyase, producing (E)-2-Hexadecenal, a derivative of sphingolipid breakdown. This compound can be oxidized to (2E)-hexadecenoic acid by long-chain fatty aldehyde dehydrogenase before being activated through linkage to coenzyme A. Notably, (E)-2-Hexadecenal induces cytoskeletal reorganization, leading to cell rounding, detachment, activation of JNK pathway targets, and ultimate apoptosis in a variety of cell types. Furthermore, it readily forms aldehyde-derived DNA adducts through reactions with deoxyguanosine and DNA.

Nicodicosapent is a fatty acid niacin conjugate. It is also an inhibitor of the sterol regulatory element-binding protein (SREBP). The sterol regulatory element-binding protein (SREBP) is a key regulator of cholesterol metabolism proteins such as PCSK9, H

Adenylosuccinic Acid Tetraammonium (also known as Adenylosuccinate or Aspartyl Adenylate) is an orally active compound that functions as a purine ribonucleoside monophosphate and is involved in nucleotide cycle metabolism. It can be transformed into fumaric acid via adenylosuccinate lyase action. This compound holds potential for research in Duchenne Muscular Dystrophy (DMD) [1].

(-)-Hydroxycitric acid (Garcinia acid) (Garcinia acid) is the principal acid of fruit rinds of Garcinia cambogia. It is a potent and competitive inhibitor of ATP citrate lyase. (-)-Hydroxycitric acid suppresses fatty acid synthesis, food intake, lipogenesis, and induced weight loss.

SHIP-2a is a cystathione γ lyase (CSE) inhibitor with IC50 value of 6.3 μM.

Abiraterone-d4 is a deuterated compound of Abiraterone. Abiraterone has a CAS number of 154229-19-3. Abiraterone (CB-7598) is an effective steroidal cytochrome P450 17alpha-hydroxylase-17, 20-lyase (CYP17) inhibitor (IC50: 4 nM).

(-)-Hydroxycitric acid (HCA) can inhibit fat synthesis and reduces food intake, the primary mechanism of action of HCA appears to be related to its ability to act as a competitive inhibitor of the enzyme ATP-citrate lyase, which catalyzes the conversion of citrate and coenzyme A to oxaloacetate and acetyl coenzyme A (acetyl-CoA), primary building blocks of fatty acid and cholesterol synthesis.

RBM10-8 irreversibly inhibits human sphingosine-1- phosphate lyase (hS1PL) while behaving also as an enzyme substrate.

Orteronel ((S)-Orteronel)(TAK-700) was selected as a candidate for clinical evaluation. orteronel (TAK-700) is currently in phase III clinical trials for the treatment of castration-resistant prostate cancer.

(-)-Hydroxycitric acid lactone (Garcinia lactone) is an anti-obesity agent.(-)-Hydroxycitric acid lactone was a potent inhibitor of ATP citrate lyase, which catalyzes the extramitochondrial cleavage of citrate to oxaloacetate and acetyl-CoA.

BACE1-IN-8 is a potent inhibitor of BACE1 (β-site APP lyase 1) (IC50: 3.9 μM).

Forrestiacid K, a terpenoid derived from Pseudotsuga forrestii, functions as an inhibitor of ATP-citrate lyase (ACL) [1].