nadh dehydrogenase

IM-156 acetate, an activator of NADH dehydrogenase (IC50=2.2 μM) and AMP-activated protein kinase alpha (AMPKα), is an orally available and bioavailable inhibitor of mitochondrial oxidative phosphorylation (OxPhos).IM-156 acetate increases AMPKα activity and inhibits chlorhexadiene-induced peritoneal fibrosis and inhibit tumor growth in rats .

Proguanil hydrochloride (Chloroquanil) is a biguanide compound which metabolizes in the body to form cycloguanil, an anti-malaria agent.Upon hydrolysis, Proguanil hydrochloride is converted to its active cyclic triazine metabolite, cycloguanil, by a cytochrome P450 dependent reaction. Cycloguanil selectively inhibits the bifunctional dihydrofolate reductase-thymidylate synthase of plasmodium parasite, thereby disrupting deoxythymidylate synthesis and ultimately blocking DNA and protein synthesis in the parasite.

ethyl 4-chloro-2-oxo-1,2-dihydroquinoline-3-carboxylate inhibits NAD(P)H: quinone oxidoreductase 1.

Pyridaben is a METI acaricide that inhibits mitochondrial electron transport at complex I (METI; Ki = 0.36 nmol/mg protein in rat brain mitochondria).

sn-Glycerol 3-phosphate, produced by the reduction of dihydroxyacetone phosphate by NADH formed during glycolysis of the cytoplasmic glycerol 3-phosphate dehydrogenase pathway.

Glycerol 3-phosphate biscyclohexylammonium salt is an endogenous metabolite produced by cytosolic glycerol 3-phosphate dehydrogenase pathway.

NADH-IN-2 (compound 8) is a Type II NADH dehydrogenase inhibitor.

NADH-IN-3 (Compound C4-1) is an NADH inhibitor with a minimum inhibitory concentration (MIC) of 4 μg/mL (13.042 μM) against the type II NADH dehydrogenase of Mycobacterium tuberculosis (Mtb). It effectively blocks ATP synthesis and demonstrates potent inhibitory effects on both single-drug (Rifampicin and Isoniazid) and multidrug-resistant (Mtb) strains, exhibiting antibacterial activity while maintaining low cytotoxicity towards HepG2 cells (SI: 16.52).

N-Desbutyl dronedarone is an active metabolite of the antiarrhythmic agent dronedarone .1,2,3It is formed from dronedarone by cytochrome P450s (CYPs) and monoamine oxidase (MAO) in human hepatocyte preparations.4N-Desbutyl dronedarone inhibits the binding of 3,3',5-triiodo-L-thyronine to the thyroid hormone receptors TRα1and TRβ1(IC50s = 59 and 280 μM for the chicken and human receptors, respectively).1It inhibits CYP2J2-mediated formation of 14,15-EET from arachidonic acid and soluble epoxide hydrolase-mediated formation of 14,15-DHET from 14,15-EET (IC50s = 1.59 and 2.73 μM, respectively, in cell-free assays).2N-Desbutyl dronedarone decreases intracellular ATP levels in H9c2 rat cardiomyocytes (IC50= 1.07 μM) and inhibits mitochondrial complex I, also known as NADH dehydrogenase, and mitochondrial complex II, also known as succinate dehydrogenase, activities in isolated rat heart mitochondria (IC50s = 11.94 and 24.54 μM, respectively).3 1.Van Beeren, H.C., Jong, W.M.C., Kaptein, E., et al.Dronerarone acts as a selective inhibitor of 3,5,3'-triiodothyronine binding to thyroid hormone receptor-α1: in vitro and in vivo evidenceEndocrinology144(2)552-558(2003) 2.Karkhanis, A., Tram, N.D.T., and Chan, E.C.Y.Effects of dronedarone, amiodarone and their active metabolites on sequential metabolism of arachidonic acid to epoxyeicosatrienoic and dihydroxyeicosatrienoic acidsBiochem. Pharmacol.146188-198(2017) 3.Karkhanis, A., Leow, J.W.H., Hagen, T., et al.Dronedarone-induced cardiac mitochondrial dysfunction and its mitigation by epoxyeicosatrienoic acidsToxicol. Sci.163(1)79-91(2018) 4.Klieber, S., Arabeyre-Fabre, C., Moliner, P., et al.Identification of metabolic pathways and enzyme systems involved in the in vitro human hepatic metabolism of dronedarone, a potent new oral antiarrhythmic drugPharmacol. Res. Perspec.2(3)e00044(2014)

sn-Glycerol 3-phosphate lithium is synthesized via the cytosolic glycerol 3-phosphate dehydrogenase pathway, involving the conversion of dihydroxyacetone phosphate to sn-Glycerol 3-phosphate using NADH generated during glycolysis.

(R)-(-)-1,2-Propanediol is a chiral isomer of 1,2-propanediol and serves as a key chiral starting material for the synthesis of chiral drugs, fine chemicals, and functional polymers; it acts as an agonist for TRPM8 in FLIPR assays (EC50 = 2.2 μM).

CBR-3465 is an inhibitor of mycobacterium tuberculosis (Mtb) type II NADH dehydrogenase. The MIC of CBR-3465 against Mtb is 0.16 μM [1].

CBR-6672, a type II NADH dehydrogenase inhibitor, demonstrates potent antimycobacterial activity against mycobacterium tuberculosis (Mtb) with a minimum inhibitory concentration (MIC) of 0.14 μM [1].

Beta-Galactose dehydrogenase catalyzes the conversion of galactose into galactonolactone, simultaneously reducing NAD to fluorescent NADH. This enzyme is useful for the determination of galactose [1].

Glucose dehydrogenase (GDH) is an oxidoreductase enzyme that facilitates the oxidation of β-D-glucose into β-D-glucono-1,5-lactone, while concurrently reducing cofactor NADP+ to NADPH, and to a lesser degree, NAD+ to NADH. It can utilize both NAD+ and NADP+ as cofactors and serves in the regeneration of NADH and NADPH [1] [2].

Glyceraldehyde phosphate dehydrogenase, targeted by anti-thymocyte and anti-apoptotic agents, catalyzes the oxidation of reduced nicotinamide adenine dinucleotide (NADH) by perhydroxyl radicals [1] [2].

6-Biotin-17-NAD+ sodium (Biotin-LC-NAD+ sodium) is a biotinylated derivative of NAD+ and can be used to measure NADH dehydrogenase activity.

HP661, a selective inhibitor of mitochondrial complex I (NADH dehydrogenase), impedes complex I activity by 77.6% at 1 µM, demonstrating lesser inhibition towards complex III (28.1%) and no inhibitory effects on complexes II and IV. It notably decreases the viability of human lung cancer cells—H460, NCI H441, and trametinib-resistant A549 cells (IC50s = 10.6, 29.7, and 15.1 nM, respectively)—which exhibit high levels of oxidative phosphorylation. In contrast, it shows minimal activity against NCI H358 lung cancer cells and non-cancerous HPNE and MRC-5 cells (IC50s = >10,000 nM for both), which have lower oxidative phosphorylation levels. Furthermore, in an H460 mouse xenograft model, HP661 at a dose of 30 mg/kg twice daily significantly reduces tumor volume and enhances the tumor-growth inhibitory effects of trametinib.

3-Acetylpyridine adenine dinucleotide functions as an alternative reductant in glutamate-synthase-catalyzed glutamate synthesis. 3-Acetylpyridine adenine dinucleotide demonstrates kinetic parameters in the AcPdADH-dependent reaction wherein Kcat and Km values for other substrates are reduced approximately fourfold relative to the NADH-dependent reaction. 3-Acetylpyridine adenine dinucleotide shows a Km of ~3 µM and acts as a competitive inhibitor of NADH in NADH-dependent glutamate synthesis with a Ki of 1 µM. 3-Acetylpyridine adenine dinucleotide provides meaningful mechanistic insights into redox cofactor selectivity in enzymatic glutamate biosynthesis.

1-Methyl-2-pentyl-4(1H)-quinolinone, a low toxic natural product containing a quinoline structure, is a specific inhibitor of Plasmodium falciparum type II NADH dehydrogenase (PfNDH2), significantly inhibits Plasmodium falciparum development in the mosquito stage and blocks malaria transmission.

2,3-Dihydroxybenzaldehyde exhibits activity against NADH dehydrogenase (Km = 35 µM) and can be used in biochemical experiments and drug synthesis.

L-Lactate Dehydrogenase, bovine muscle, is a redox enzyme that catalyzes the reversible conversion of lactate to pyruvate while simultaneously reducing NAD+ to NADH.