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 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-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.

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.

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.

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.

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.

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].

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.