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.

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.

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.

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.

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-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 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.

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

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.

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

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

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 an inhibitor of LDHA that acts by reducing lactate production in HeLa cells.

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

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].

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.

WQQ-345, a BCAT1 inhibitor, exhibits an IC50 of 10.8 mM. In 67R cells, it reduces α-KG levels and upregulates H3K27me3 expression while downregulating the expression of glycolytic enzymes (PFKP and LDHA), leading to impaired glycolytic activity. Additionally, WQQ-345 demonstrates tumor-suppressive activity in a 67R subcutaneous xenograft model.