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

ALDH2 modulator 1 is a potent and orally active modulator of acetaldehyde dehydrogenase-2 (ALDH2), which reduces blood alcohol levels in mice.

ALDH1A3-IN-2 is a potent ALDH1A3 inhibitor with an IC50 of 0.30 μM.ALDH1A3-IN-2 has potential for cancer disease research.

5-(2-Furyl)-2-hydroxybenzoic acid is an inhibitor of glycolate oxidase (GO) and can be used to study metabolism-related disorders such as primary hyperoxaluria type 1 (PH1).

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

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.

N-[2-(5-Chloro-1H-indol-3-yl)ethyl]-4'-cyanobiphenyl-2-carboxaMide, a TAU cytotoxicity inhibitor, inhibits LDH leakage of M17-TAU P301L cells with EC50 of 325nM.

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.

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.

ALDH1A3-IN-1 (Compound 14) is a potent inhibitor of ALDH1A3 which can be used in prostate cancer research (IC50 = 0.63 μM; Ki = 0.46 μM) [1].

ALDH3A1-IN-2 (Compound 19), a potent inhibitor of aldehyde dehydrogenases (ALDHs), demonstrates high efficacy against ALDH3A1 with an IC50 of 1.29 μM. Given the overexpression of ALDHs in multiple tumor types, including prostate cancer, ALDH3A1-IN-2 holds significant potential for cancer research [1].

LDHA/PDKs-IN-1 (compound 20e) is a highly effective dual inhibitor of PDKs and LDHA, displaying IC50 values of 0.8 μM and 0.15 μM, respectively. It significantly suppresses A549 cell proliferation (EC50 = 13.2 μM), reduces lactate formation, and enhances oxygen consumption. This compound holds great promise for cancer research [1].

LDHA/PDKs-IN-2 (compound 20k) is a potent LDHA and PDKs dual inhibitor with IC50 values of 0.7 and 1.6 μM, respectively. LDHA/PDKs-IN-2 increases oxygen consumption as well as decreases the lactate formation. LDHA/PDKs-IN-2 shows the potential for the cancer research which reduces the proliferation of A549 cell with an EC 50 of 15.7 μM [1].

ALDH1A3-IN-3 (compound 16), a powerful ALDH1A3 inhibitor with an IC50 of 0.26 μM, serves as an effective ALDH3A1 substrate. It is utilized in prostate cancer research.

ALDH1A1-IN-3 is a good and selective inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1) (IC50: μM).ALDH1A1-IN-3 is effective in improving glucose consumption in HepG2 cells.ALDH1A1-IN-3 can be used for studies to improve glucose metabolism.

ALDH1A1-IN-2 is a potent aldehyde dehydrogenase 1a1 (aldh1a1) inhibitor with anticancer activity.ALDH1A1-IN-2 may be used in the study of breast cancer, inflammation or obesity.

ALDH1A2-IN-1 is a reversible inhibitor of the active site of ALDH1A2, showing a significant affinity for the enzyme with an IC50 value of 0.91 μM and a Kd value of 0.26 μM. This compound interacts hydrophobically with the enzyme, contributing to its inhibitory properties.

ALDH3A1-IN-1 is a small molecule ALDH3A1 inhibitor, (IC50:1.61 μM), which can be used for the study of hyperprolinemia and dry-Larsen syndrome.

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

MS6105 is a chimeric LDH protein hydrolysis-targeted PROTAC that degrades LDHA and LDHB efficiently, with its activity contingent on both time and the ubiquitin-proteasome system, exhibiting anticancer properties [1]. Additionally, as a click chemistry reagent possessing an Alkyne group, MS6105 can partake in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions with Azide-bearing molecules.

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.

1. Ilexsaponin A (Ilexsaponin A1) shows protective effects on ischemia-reperfusion-induced myocardial injury through anti-apoptotic pathway.

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.

6''-O-Acetylglycitin is a potential nutriceutical, it is also a potent LDH inhibitor.

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).

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).

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.

(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.

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.

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].

LDCA is a double-hit metabolic regulator that exhibits potent anti-proliferative activity. lDCA competitively inhibits LDH-A enzyme activity, alters mitochondrial hyperpolarization and simultaneously subverts apoptosis. lDCA has a pronounced effect in cancer cells and does not show toxicity.

Glomeratose A is a lactate dehydrogenase inhibitor.

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.

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).

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

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.

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)

D-Tetrahydropalmatine is a organic cation transporter 1 (OCT1) inhibitor, it can obviously inhibit the uptake of monocrotaline (MCT) in MDCK-hOCT1 cells and isolate rat primary hepatocytes, and attenuate the viability reduction and LDH release of the prim

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.

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.

Boc-Asp(OMe)-fluoromethyl ketone (Boc-Asp(OMe)-FMK) is a broad range caspase inhibitor. Boc-Asp(OME)-Fluoromethyl Ketone inhibits Fas-mediated phagocytosis and oxidative rupture inhibition, but does not affect the chemotactic activity of IL-8.

(-)-Eseroline fumarate, a metabolite of the acetylcholinesterase inhibitor Physostigmine, promotes lactic acid dehydrogenase (LDH) leakage from cancer cells and triggers adenine nucleotides and 5-hydroxytryptamine (5-HT) release from neuronal cells, leading to cell death. Additionally, it suppresses electrically evoked muscle contractions in the mouse vas deferens and the guinea-pig ileum.

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].

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

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).

B355252 protects against cell death caused by glutamate-evoked oxidative stress. B355252 shows neuroprotective effect, potentiating nerve growth factor (NGF)-induced neurite outgrowth.

Sodium Oxamate (Oxamic acid sodium salt) is an LDH inhibitor that specifically inhibits LDHA. Sodium Oxamate has antitumor activity and induces cell cycle arrest and apoptosis.

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

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