LDHA Inhibitor

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.

FX-11 (LDHA Inhibitor FX11) is a highly potent, selective, and competitive inhibitor of lactate dehydrogenase A (LDHA), with a Ki value of 8 μM for LDHA. FX-11 acts as an activator of PKM2 (pyruvate kinase M2). FX-11 exerts its antitumor effects by inhibiting glycolysis, depleting ATP, and inducing oxidative stress and apoptosis. FX-11 can be used in tumor metabolism research.

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.

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.

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.

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.

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

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.

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.

Oxamic acid is an LDHA (lactate dehydrogenase A) inhibitor with antitumor activity that induces cancer cell apoptosis, downregulates EGFR expression, and inhibits cancer stem cell properties and EMT.

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.

ZG-2492 is an orally active LDHA inhibitor with an IC50 value of 156 nM. It reduces lactate production in pancreatic cancer cells and induces cell cycle arrest and apoptosis (apoptosis). ZG-2492 exhibits antitumor activity and is applicable for research in pancreatic and other types of cancer.

LDHA-IN-10 (Compound HP19) is an inhibitor of lactate dehydrogenase A (LDHA) with an IC50 value of 5.2 μM. It reduces lactate production and ATP levels, inhibiting the proliferation of the pancreatic cancer cell line PANC-1. Additionally, LDHA-IN-10 induces G1/S cell cycle arrest and promotes apoptosis, showing potential for research in pancreatic ductal adenocarcinoma (PDAC).

Dual GO/LDHA-IN-1 is an orally effective dual-target inhibitor of glycolate oxidase (GO) and lactate dehydrogenase A (LDHA), with Ki values of 390 nM and 40 nM, respectively. It decreases liver LDHA levels, urinary oxalate excretion, and renal calcium oxalate crystal deposition. Dual GO/LDHA-IN-1 is applicable for research in primary hyperoxaluria type 1.

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 is a novel and potent lactate dehydrogenase A (LDHA) inhibitor that disrupts glycolytic metabolism in MIA PaCa-2 human pancreatic cancer cells, inducing rapid metabolic reprogramming prior to delayed cell death, with intrinsic resistance observed in OXPHOS-dependent pancreatic cell lines that can be reversed by phenformin, while acquired resistance is driven by AMPK-mTOR-S6K pathway activation, highlighting its value for studying metabolic plasticity and therapeutic resistance.

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

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.

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].