Lactate Dehydrogenase Inhibitor

3-Acetylpyridine adenine dinucleotide, 90% (3-APAD, 90%; 3-Acetylpyridine NAD, 90%) is an analog of nicotinamide adenine dinucleotide (NAD). 3-Acetylpyridine adenine dinucleotide, 90% synergizes with sulfite to inhibit lactate dehydrogenase (LDH) .

(S)-GNE-140 (Compound 30-S) is the S enantiomer of GNE-140 (HY-118241). (S)-GNE-140 is a potent inhibitor of human LDHA and LDHB, with IC₅₀ values of 55 nM and 140 nM, respectively. (S)-GNE-140 exerts its inhibitory effect by non-competitively binding to NADH and occupying the LDH pyruvate site, but its activity is weaker than that of the R enantiomer. (S)-GNE-140 can be used for cancer research.

Nifurtimox, an antiprotozoal agent, which is generally used for the treatment of infections with Trypanosoma cruzi, has been used in the therapy of neuroblastoma. Nifurtimox affects enzyme activity of lactate dehydrogenase (LDH).

Licoflavone A is an orally active PTP1B/VEGFR-2 inhibitor, with an IC₅₀ of 54.5 μM against PTP1B, an IC₅₀ of 14.36 μM and a K_d of 142.38 nM against human VEGFR-2. Licoflavone A blocks the PI3K/AKT and MEK/ERK signaling pathways. Licoflavone A induces G1 phase cell cycle arrest, apoptosis via the intrinsic mitochondrial pathway (apoptosis), and inhibits migration, invasion and epithelial-mesenchymal transition (EMT) of gastric cancer cells. Licoflavone A inhibits the proliferation of gastric cancer cells in vitro and in xenograft models. Licoflavone A reduces the expression levels of HIF-1α, GLUT1, LDHA, PKM2 and HK2 in hypoxic gastric cancer cells, decreases glucose uptake and suppresses glycolysis. Licoflavone A can be used in research related to gastric cancer, type 2 diabetes and obesity.

3′,4′,7-Trihydroxyflavone is an orally active inhibitor of OXA-48 (IC₅₀ = 1.89 μM) and COX-1 (IC₅₀ = 36.37 μM). 3′,4′,7-Trihydroxyflavone exhibits antioxidant and anti-inflammatory properties, inhibiting the release of inflammatory cytokines such as IL-6, IL-8, and TNF-α. 3′,4′,7-Trihydroxyflavone inhibits H₂O₂-induced neuronal apoptosis and ROS accumulation, and exerts anti-neuroinflammatory effects by suppressing the JNK-STAT1 pathway. 3′,4′,7-Trihydroxyflavone exhibits antimicrobial and antibiotic-modifying activities against multidrug-resistant Gram-negative enteric bacteria. 3′,4′,7-Trihydroxyflavone inhibits RANKL-induced osteoclast formation via NFATc1. 3′,4′,7-Trihydroxyflavone activates the CREB-BDNF axis and restores scopolamine (HY-N0296)-induced memory deficits in mice.

CHK-336 (Example 1) is an orally active LDHA inhibitor (IC₅₀<1 nM). CHK-336 inhibits lactate production in mouse hepatocytes. CHK-336 can be used in the study of hyperoxaluria.

NHI-2 is a lactate dehydrogenase A (LDHA) inhibitor with an IC₅₀ of 14.7 µM. NHI-2 shows selective for LDHA over LDHB (IC₅₀ = 55.8 µM). NHI-2 is an efficient anti-glycolytic agent. NHI-2 enhances apoptosis, induces cell cycle arrest at S and G2 phases. NHI-2 has a broad spectrum anti-proliferative activity in cancer cells. NHI-2 affects extracellular acidification rate and ATP production. NHI-2 suppresses tumor growth in murine B78 melanoma tumor model.

Rehmannioside A is a compound that can be isolated from Rehmanniae radix. Rehmannioside A is an inhibitor of CYP3A4, 2C9 and 2D6, with IC₅₀ values of 10.08, 12.62 and 16.43 μM, respectively. Rehmannioside A has anti-inflammatory, antioxidant, anti-apoptosis, anti-ferroptosis, cognitive improvement and neuroprotective activities. Rehmannioside A can be used for the research of nervous system and inflammation-related diseases.

3-​Dehydrotrametenolic acid, isolated from the sclerotium of Poria cocos, is a lactate dehydrogenase (LDH) inhibitor. 3-​Dehydrotrametenolic acid promotes adipocyte differentiation in vitro and acts as an insulin sensitizer in vivo. 3-​Dehydrotrametenolic acid induces apoptosis and has anticancer activity.

Glomeratose A is a lactate dehydrogenase inhibitor, isolated from Polygala tenuifolia.

2-Oxovaleric acid (Standard) is the analytical standard of 2-Oxovaleric acid (HY-113098). This product is intended for research and analytical applications. 2-Oxovaleric acid is an analog of Pyruvate and a substrate inhibitor of Lactate dehydrogenase, exhibiting substrate inhibitory activity against lactate dehydrogenase from Phycomyces blakesleeanus.

Vitexin-4''-O-glucoside (4''-O-Glucosylvitexin) is an orally active natural flavonoid component with multiple pharmacological effects including antioxidation, anti-inflammation, cytoprotection and anti-apoptosis. Vitexin-4''-O-glucoside regulates the MAPK signaling pathway by downregulating the phosphorylation levels of JNK and p38, thereby blocking endoplasmic reticulum stress responses. Vitexin-4''-O-glucoside alleviates oxidative stress by reducing MDA content and upregulating the activities of SOD and CAT, attenuates inflammation by downregulating the expressions of inflammatory factors TNF-α, IL-1β and IL-6, and also reduces LDH release and inhibits caspase-3 activation. Vitexin-4''-O-glucoside effectively improves drug-induced acute liver injury and exerts significant protective effects against myocardial hypoxia/reoxygenation injury. Vitexin-4''-O-glucoside can be used in studies on acute liver injury, cardiovascular diseases and myocardial hypoxia-reoxygenation injury.

Nedosiran (DCR-PHXC) is an RNA interference (RNAi) targeting lactate dehydrogenase (LDH). Nedosiran represents an impactful potential therapeutic for primary hyperoxaluria (PH) with end-stage renal disease (ESRD). Nedosiran is a GalNAc-dsRNA conjugate.

MEDS433 is a potent inhibitor of human dihydroorotate dehydrogenase (hDHODH) with an IC₅₀ of 1.2 nM. MEDS433 exerts a potent antiviral activity against RSV-A and RSV-B in the one-digit nanomolar range. MEDS433 induces the expression of antiviral proteins encoded by interferon stimulated genes (ISGs) able to reduce RSV replication.

LDCA is a dual-hit metabolic modulator and inhibits LDH-A enzyme activity to stimulate apoptosis in the malignant population. LDCA can be used for the research of oncogenic progression.

LDHA-IN-7 (compound 21) is an oral bioactive inhibitor of lactate dehydrogenase-A (LDHA) and LDHB, with the IC₅₀s of 72 nM and 1.2 Μm, respectively.

(±)-Liquiritigenin ((±)-4',7-Dihydroxyflavanone) is a dihydroflavone flavonoid. (±)-Liquiritigenin is isolated from the aerial parts of Angelica keiskei. (±)-Liquiritigenin reduces LDH release in cells. (±)-Liquiritigenin exerts a cytoprotective effect against glucose oxidase-induced cellular oxidative stress. (±)-Liquiritigenin exhibits a tumor-promoting effect in liver cancer.

GNE-140 (Compound 28) is an external racemic mixture of (R)-GNE-140 (HY-100742A) and (S)-GNE-140 (HY-100742B). GNE-140 is an effective lactate dehydrogenase (LDH) inhibitor, with the IC₅₀ values for LDHA and LDHB being 9 nM and 30 nM respectively. GNE-140 can be used in cancer research.

Lathosterol (Standard) is the analytical standard of Lathosterol (HY-113486). This product is intended for research and analytical applications. Lathosterol is a plant sterol and cholesterol-like molecule. Lathosterol increases antioxidant enzymes (such as SOD, CAT, and GSH) and decreases LDH. Lathosterol has a hepatoprotective effect on mice with acetaminophen (HY-66005)-induced liver injury^[1].

3-Acetylpyridine adenine dinucleotide, 95% (3-APAD, 95%)is an analog of nicotinamide adenine dinucleotide (NAD). 33-Acetylpyridine adenine dinucleotide, 95% collaboratively inhibits Lactate Dehydrogenase (LDH) with bisulfite.