LDHA

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.

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.

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.

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

(S)-GNE-140 is the less active enantiomer of GNE-140.

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.

GSK2837808A is a potent and selective inhibitor of lactate dehydrogenase A (LDHA) with IC50 values of 1.9 nM for LDHA and 14 nM for LDHB.

LDHA-IN-8, a small molecule inhibitor of lactate dehydrogenase A (LDHA), inhibits the proliferation of pancreatic and lung cancer cells by inhibiting the activity of LDHA-catalyzed pyruvate in a dose-dependent manner (EC 50=14.54μM), decreasing the intracellular lactate content and increasing the intracellular reactive oxygen species (ROS) levels.

LDHA-IN-9 (Compound 1g) is an LDH-A inhibitor with an IC50 of 25 nM. It inhibits the proliferation of DLD-1 cells by inducing apoptosis, with a GI50 of 27 μM. In mouse models, LDHA-IN-9 exhibits antitumor activity without significant toxicity at a dose of 25 mg kg.

LDHA-IN-6 (compound 6) is an orally active inhibitor of lactate dehydrogenase A (LDHA) with an IC50 of 46 nM, demonstrating antitumor activity.

LDHA-IN-7 (compound 21) is an orally active inhibitor targeting lactate dehydrogenase A (LDHA) and LDHB, with IC50 values of 72 nM and 1.2 μm, respectively.

LDHA/PDKs-IN-2 (compound 20k) is a potent dual inhibitor of LDHA and PDKs, with IC50 values of 0.7 and 1.6 μM, respectively. It increases oxygen consumption, decreases lactate formation, and shows potential for cancer research by reducing the proliferation of A549 cells with an EC50 of 15.7 μM [1].

LDHA/PDKs-IN-1 (compound 20e) is a highly effective dual inhibitor of PDKs and LDHA, with 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, holding great promise for cancer research [1].

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.

L-Lactic acid ((S)-2-Hydroxypropanoic acid) is a natural product produced by the anaerobic glycolysis of pyruvic acid. L-Lactic acid is a sensitive indicator of tissue hypoxia and can be used as a hemodynamic indicator in critically ill patients.

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.

Triflupromazine is a dopamine receptor D1 D2 antagonist and LHDA inhibitor that suppresses dopamine activity in the central nervous system (CNS) and promotes LDHA-mediated AMBRA1 ubiquitination, used for treating mental disorders, sedation, and antiemesis.

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 is a lactate dehydrogenase inhibitor that inhibits the activity of lactate dehydrogenase. Galloflavin inhibits both human LDH isoforms (type A and type B) by preferentially binding to the free enzyme without competing with substrates or cofactors, with Ki values ​​calculated by pyruvate of 5.46 μM (LDH-A) and 15.06 μM (LDH-B).

NHI-2 is a lactate dehydrogenase A (LDHA) inhibitor with an IC50 value of 14.7 µM, demonstrating high selectivity for LDHA over LDHB, for which the IC50 is 55.8 µM. NHI-2 functions as an efficient anti-glycolytic agent, enhancing apoptosis, inducing cell cycle arrest at the S and G2 phases, and exerting broad-spectrum antiproliferative effects in cancer cells. NHI-2 additionally affects extracellular acidification rates and ATP production and has demonstrated tumor growth suppression in murine B78 melanoma models, highlighting its role in cancer metabolism research.

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

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

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].

CHK-336 (Example 1), an orally active LDHA inhibitor (IC50 <1 nM), suppresses lactate production in mouse hepatocytes and is applicable in hyperoxaluria research [1].