lactate dehydrogenase

L-Lactate dehydrogenase, a redox enzyme, catalyzes the in vivo reduction of pyruvate to L-lactate with absolute enantiospecificity by utilizing NADH [1].

D-Lactate dehydrogenase (D-LDH), an oxidoreductase, catalyzes the oxidation of D-lactate to pyruvate leveraging NAD+ or NADP+ as acceptors and acting on the donor CH-OH group. Predominantly found in bacteria and fungi, it is frequently utilized in biochemical research [1].

(L)-Sodium lactate (Sodium L-Lactate) is produced from pyruvate by the enzyme Lactate Dehydrogenase. Lactate production occurs during anaerobic glycolysis or in proliferatively active cells. L-Lactic Acid occurs in small quantities in the blood and muscle fluid of man and animals. The lactic acid concentration increases in muscle and blood after vigorous activity. L-Lactic acid is also present in liver, kidney, thymus gland, human amniotic fluid, and other organs and body fluids.

Isomalt (Palatinitol) is a mixture of 1,6-mannitol glucopyranoside and 1,6-sorbitol glucopyranoside

GSK2837808A is a potent and selective inhibitor of lactate dehydrogenase A (LDHA) (IC50s: 1.9 and 14 nM for LDHA and LDHB, respectively).

LDH-IN-1 is a pyrazole-based human lactate dehydrogenase (LDH) inhibitor(IC50s of 32 and 27 nM for LDHA and LDHB, respectively).

Nifurtimox (BAY-A-2502) is an antiprotozoal agent (IC50s = 9.91, 12.28, and 10.44 μM against Taluahuén, LQ, and Brener strains of T. cruzi- epimastigotes, respectively).

(R)-GNE-140 (GNE-140) is an effective LDHA/LDHB inhibitor (IC50s: 3/5 nM) and is 18-fold more potent than S enantiomer.

Compound CMC23, an FPR2 agonist, mitigates lactate dehydrogenase release in LPS-stimulated cultures and reduces pro-inflammatory IL-1β and IL-6 levels. It also attenuates phosphor-STAT3 levels through the STAT3/SOCS3 signaling pathway [1].

Nedosiran sodium, a GalNAc-dsRNA conjugate, is engineered to suppress the synthesis of the hepatic lactate dehydrogenase (LDH) enzyme.

PfDHODH-IN-1 is an analogue of the active Leflunomide metabolite, has antimalarial activity.

3-Butynoic acid is a potent inhibitor of acyl CoA dehydrogenase, a substrate for the Zn-dependent flavoproteinase D-lactate dehydrogenase, and can be used to study lactic acid metabolism.

Nedosiran (DCR-PHXC) is a GalNAc-dsRNA conjugate designed for RNA interference (RNAi) targeting lactate dehydrogenase (LDH). It serves as a potential therapeutic option for patients with primary hyperoxaluria (PH) and end-stage renal disease (ESRD).

GNE-140 is a potent inhibitor of lactate dehydrogenase A (LDHA). GNE-140 is a racemate mixture of (R)-GNE-140 and (S)-GNE-140.

Galloflavin Potassium is an inhibitor of lactate dehydrogenase.

RS6212 is a specific lactate dehydrogenase (LDH) inhibitor (IC50=12.03 μ M）。 RS6212 shows strong anticancer activity in a variety of cancer cell lines.

Glomeratose A is a lactate dehydrogenase inhibitor.

Kakkalide is a potent lactate dehydrogenase (LDH) inhibitor, it has anti-inflammatory effects.

Thevetiaflavone (2-Genistein-5-methyl ether) is a natural flavonoid from Wikstroemia indica that inhibits the leakage of lactate dehydrogenase from the cytoplasm and increases cell viability.

LDHA-IN-5 is a novel and potent inhibitor targeting both glycolate oxidase (GO) and lactate dehydrogenase A (LDHA), designed for the treatment of primary hyperoxaluria.

4-(Dimethylamino)phenol enhances extracellular lactate dehydrogenase (LDH) levels without significant effects on gluconeogenesis. Only when the membrane becomes permeable to LDH does 4-(Dimethylamino)phenol reduce ATP content.

NCI-006 is a potent new inhibitor of lactate dehydrogenase (LDH) that disrupts tumor growth in mice. LDH inhibition slows tumor growth but rapidly redirects pyruvate to support mitochondrial metabolism. Inhibiting both mitochondrial complex 1 and LDH suppresses metabolic plasticity of glycolytic tumors in vivo, significantly prolonging tumor growth inhibition.

Iristectorin A, an isoflavone compound derived from Iris tectorum Maxim, is a lactate dehydrogenase inhibitor that is used in cancer research.

(E)-2-(2-Chlorostyryl)-3,5,6-trimethylpyrazine (CSTMP) is a stilbene derivative with antioxidant and anticancer activities. It stimulates proliferation of hydrogen peroxide-damaged ECV-304 cells (EC50 = 24.9 nM). CSTMP reduces hydrogen peroxide-induced release of lactate dehydrogenase (LDH) in and increases viability of human umbilical vein endothelial cells (HUVECs) in a concentration-dependent manner via inhibition of apoptosis. It reverses hydrogen peroxide-induced release of malondialdehyde (MDA) and decreases in superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) activities as well as increases constitutive nitric oxide synthase (cNOS) activity and nitric oxide (NO) production in HUVECs. CSTMP also induces cell death of A549 non-small cell lung cancer (NSCLC) cells in an IRE1α-dependent manner through induction of IRE1α-TRAF2-ASK1 complex-mediated endoplasmic reticulum (ER) stress and mitochondrial apoptosis.

Sodium 2-hydroxybutanoate (alpha-hydroxybutyrate) is formed as a by-product of the formation of alpha-ketobutyrate via a reaction catalyzed by lactate dehydrogenase (LDH) or alpha-hydroxybutyrate dehydrogenase (alphaHBDH).

Tenuifoliside C, isolated from polygala tenuifolia willd, is a target lactate dehydrogenase inhibitor. It significantly inhibits chlorzoxazone 6-hydroxylation catalyzed by CYP2E1[1].

Sibiricose A5 is a lactate dehydrogenase inhibitor, it displays antidepressant-like, and antioxidant actions. Sibiricose A5 can protect PC12 cells damage induced by P. tenuifolia.

EP2 receptor antagonist-2 (CID891729) is a compound that not only serves as an antagonist to the EP2 receptor, blocking its activation by PGE2, but also reduces lactate dehydrogenase (LDH) release triggered by N-methyl-D-aspartate (NMDA).

JC2-11 is an inhibitory compound for inflammation.JC2-11 inhibits the recruitment domain-containing proteins NLRC 4, atypical in melanoma 2 (AIM 2) and atypical (NC) inflammatory vesicles by disrupting reactive oxygen species (ROS) production and caspase-1 activity.JC2-11 reduces caspase-1 (p20) secretion, gasdermin D (GSDMD) cleavage, IL-1β and lactate dehydrogenase (LDH) activity in inflammatory vesicles. JC2-11 reduced caspase-1 (p20) secretion, gasdermin D (GSDMD) cleavage, IL-1β and lactate dehydrogenase (LDH) release from inflammatory vesicles.

11-Keto-beta-boswellic acid, a novel Nrf2 activator, and a selective 5-lipoxygenase (5-LOX) inhibitor; it exerts dose dependent cardioprotective effect manifested by dose-dependent reduction in serum lactate dehydrogenase

(S)-2-Hydroxy-3-phenylpropanoic acid (L-(−)-3-Phenyllactic acid) is a chiral aromatic compound involved in phenylalanine metabolism. It is likely produced from phenylpyruvate via the action of lactate dehydrogenase. The D-form of this organic acid is typically derived from bacterial sources while the L-form is almost certainly endogenous. Levels of phenyllactate are normally very low in blood or urine. High levels of PLA in the urine or blood are often indicative of phenylketonuria (PKU) and hyperphenylalaninemia (HPA). PKU is due to lack of the enzyme phenylalanine hydroxylase (PAH) so that phenylalanine is converted not to tyrosine but to phenylpyruvic acid (a precursor of phenylacetate).

Nigerose, a disaccharide identified in Acremonium, effectively maintains stability in HL-60 cells post-cryopreservation by preventing elevations in malondialdehyde (MDA) and reactive oxygen species (ROS) levels, and inhibiting lactate dehydrogenase (LDH) release, when administered at a 150 µM concentration alongside the glycoside salidroside.

1. 3-Dehydrotrametenolic acid can be a potential anticancer agent against H-ras transformed tumor. 2. Dehydrotrametenolic acid is a promising candidate for a new type of insulin-sensitizing drug.

FX-11 (LDHA Inhibitor FX11) is A potent, selective and competitive specific inhibitor of lactate dehydrogenase A (LDHA) with a Ki of 8 μM. FX-11 can activate PKM2 (pyruvate kinase M2). FX-11 can reduce ATP levels, induce oxidative stress and ROS production, and cause cell death. FX-11 appeared antitumor activity during xenotransplantation of lymphoma and pancreatic cancer.

CAY10762 is an inhibitor of monoacylglycerol lipase (MAGL; IC50= 34.1 nM).1It reduces hydrogen peroxide-induced lactate dehydrogenase (LDH) release from Neuro2a cells when used at a concentration of 1 μM. CAY10762 (10 mg/kg) increases levels of 2-arachidonoyl glycerol in mouse brain. 1.Castelli, R., Scalvini, L., Vacondio, F., et al.Benzisothiazolinone derivatives as potent allosteric monoacylglycerol lipase inhibitors that functionally mimic sulfenylation of regulatory cysteinesJ. Med. Chem.63(3)1261-1280(2020)

Tenuifoliside B is a natural product from the roots of Polygala tenuifolia.And is a target lactate dehydrogenase inhibitor. Tenuifoliside B has cognitive improving and cerebral protective effects. it can inhibit potassium cyanide (KCN)-induced hypoxia and scopolamine-induced memory impairment in mice.

LDHA-IN-3 (1-(phenylseleno)-4-(trifluoromethyl) benzene) is a potent non-competitive lactate dehydrogenase (LDHA) inhibitor with an IC50 value of 145.2 nM.LDHA-IN-3 is a selenobenzene compound that can be used in cancer research.

Anticancer agent 122, a potent inhibitor of human lactate dehydrogenase A (h LDHA), exhibits significant anticancer activities, rendering it suitable for use in cancer research [1].

Zofenoprilat, an angiotensin-converting enzyme (ACE; IC50 = 8 nM for rabbit lung enzyme) inhibitor and the active metabolite of the prodrug zofenopril, effectively counters angiotensin I- or bradykinin-induced contractions in isolated guinea pig ileum (EC50s = 3 and 1 nM, respectively). At a concentration of 10 nM, Zofenoprilat not only diminishes basal endothelin-1 secretion and nitric oxide (NO) production but also safeguards against TNF-α-stimulated increases in reactive oxygen species (ROS) and reductions in glutathione (GSH) levels within human umbilical vein endothelial cells (HUVECs). Furthermore, at 10 µM, it delivers protection to primary human cardiac microvascular endothelial cells from doxorubicin-induced toxicity and enhances hydrogen sulfide (H2S) production, along with the adhesion, migration, and proliferation of HUVECs. Additionally, Zofenoprilat (400 µM) mitigates end diastolic pressure and lactate dehydrogenase (LDH) release, demonstrating therapeutic potential in a Langendorff isolated perfused rat heart model of ischemia-reperfusion injury.

Meclocycline is a tetracycline antibiotic with broad antimicrobial activity. Meclocycline inhibits lactate dehydrogenase (LDH) release and cell toxicity induced by expression of htt-N63-148Q, a mutant form of the huntingtin gene, without altering htt-N63-148Q protein levels in PC12 cells.

hDHODH-IN-1 is a human dihydroorotate dehydrogenase (hDHODH) inhibitor with an anti-inflammatory effect.

NCATS-SM1440 is a Lactate Dehydrogenase Inhibitor with Optimized Cell Activity and Pharmacokinetic Properties.

Antioxidant agent-3 (Compound 14q), a potent antioxidant, exhibits strong scavenging activity against DPPH radicals and ABTS+ radicals, with IC50 values of 26.58 μM and 30.31 μM, respectively. Additionally, it enhances the levels of reactive oxygen species (ROS), superoxide dismutase (SOD), and glutathione (GSH), while diminishing lactate dehydrogenase (LDH) in H2O2-treated HepG2 cells [1].

GNE-140 racemic is a potent lactate dehydrogenase (LDHA) inhibitor.

Anticancer agent 121, a human lactate dehydrogenase A (hLDHA) inhibitor, exhibits potent anticancer activities, suitable for use in anticancer research [1].

6(5H)-Phenanthridinone is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2. It decreases radiation-induced PARP activity and proliferation of RDM4 murine lymphoma cells. 6(5H)-Phenanthridinone reduces NF-κB-induced transcription of the genes encoding TNF-α, IL-2, and IFN-γ in rat lymphocytes. In vivo, 6(5H)-phenanthridinone reduces spinal cord expression of inducible nitric oxide synthase (iNOS), IL-1β, TNF-α, IL-2, and IFN-γ and reduces disease score in a rat model of experimental autoimmune encephalomyelitis (EAE). It also decreases serum levels of lactate dehydrogenase as well as hepatic lipid peroxidation, oxidative DNA damage, and PARP levels.

LDHA-IN-4 (AZ33) is an LDHA inhibitor. Binding affinity to 6-His-tagged human LDHA (2 to 322 amino acid residue) expressed in Escherichia coli BL21 (DE3) cells by SPR analysis with an active value of 0.093 μM.

Clofibric acid-d4 is intended for use as an internal standard for the quantification of clofibric acid by GC- or LC-MS. Clofibric acid is a peroxisome proliferator-activated receptor α (PPARα) agonist (EC50 = 50 µM in a transactivation assay) and the active metabolite of clofibrate. It is formed from clofibrate by tissue and serum esterases. Dietary administration of clofibric acid (0.067-0.22%) reduces serum cholesterol, phospholipid, and triglyceride levels in rats. It decreases glutamate oxaloacetate transaminase (GOT) levels and increases glutamate pyruvate transaminase (GPT) and lactate dehydrogenase (LDH) levels, markers of xenobiotic stress, in the plasma of carp (C. carpio) when administered in tank water at a concentration of 10 µg/L. Clofibric acid has been found in wastewater effluent.

N-Methyl-D-aspartate (NMDA) receptors are Ca2+ permeable ligand-gated channels of the central nervous system that are activated after binding of the co-agonists glutamate and glycine. CAY10608 is a propanolamine that potently, selectively, and non-competitively antagonizes the NR2B subunit of NMDA receptors (IC50 = 50 nM). It does not inhibit NR1, NR2A, NR2C, and NR2D subunits and has no significant effects on α-amino-3-hydroxy-5-methyl-4-isoxazolepropioinic acid (AMPA) or kainate receptors. CAY10608 is neuroprotective, since it prevents NMDA-triggered release of lactate dehydrogenase from cultured cortical neurons. Also, CAY10608, when administered intraperitoneally, reduces brain infarct volume resulting from transient ischemia via carotid artery occlusion.

Galloflavin inhibits both the A and B isoforms of lactate dehydrogenase with Ki of 5.46 µM and 15.06 µM, respectively. Galloflavin is also a potential anticancer agent.

Clofibric acid (Chlorofibrinic acid) is an antilipemic agent that is the biologically active metabolite of CLOFIBRATE.