depletion

6-Aminonicotinamide (6-AN) is a well-established inhibitor of the NADP+-dependent enzyme.

Alemtuzumab is a humanized monoclonal antibody against CD52 an antigen found on the surface of normal and malignant lymphocytes.

Imidazole ketone erastin (IKE) is an ferroptosis inducer with inhibitory effects on system Xc-cystine/glutamate transporter proteins. Imidazole ketone erastin has antitumor activity and induces glutathione depletion and lipid peroxidation.

Sotuletinib (BLZ945) is a CSF-1R inhibitor, a highly selective, brain-penetrant CSF-1R inhibitor (IC50 = 1 nM, with 1000-fold selectivity over other kinases), with oral activity, used for microglia depletion and tumor and neurological disease research.

5-Ph-IAA is an IAA derivative and a highly efficient, low-toxicity, reversible protein degradation ligand specifically designed for the AID2 system. AID2 induces rapid and effective depletion of mAID fusion proteins, enabling the study of protein function in living cells; it also exhibits antitumor activity. 5-Ph-IAA can be used in antitumor research.

Sulfo-ara-F-NMN is an analogue of nicotinamide mononucleotide (NMN) with cellular permeability. Sulfo-ara-F-NMN was selective to activate SARM1 and inhibited CD38 with an IC50 of about 10 μM. Activation by Sulfo-ara-F-NMN to Z-48 or NMN, which has a higher cyclase activity, causes conformational changes in SARM1, resulting in cADPR production, NAD depletion, and non-apoptotic cell death.

Losulazine is a peripheral sympathetic antihypertensive compound that can be taken orally. Losulazine causes relatively modest, transient depletion of dopamine and norepinephrine in brain regions protected by the blood-brain barrier.

Reserpine (Serpalan) is an alkaloid isolated from the root of Rauwolfia serpentina. As an inhibitor of vesicular monoamine transporter 2 (VMAT2), it suppresses the uptake of norepinephrine into storage vesicles, leading to depletion of catecholamines and serotonin in central and peripheral nerve terminals. It has antihypertensive and antipsychotic effects and can be used to induce gastric ulcer and depression models.

Tinidazole (CP12574)a is a 5-nitroimidazole derivative with the antiprotozoal property. Although the mechanism of action has not been fully elucidated, it has been suggested that tinidazole is metabolized and yields nitrite anions and metronidazole. Metronidazole's nitro group, in turn, is reduced via the parasite ferredoxin, thereby generating a series of free nitro radicals including nitro anions. Toxicity is achieved via depletion of sulfhydryl groups and DNA strand breaks with multiple hits having an additive effect and ultimately leading to cell death.

Ammonium formate (Formic acid ammonium salt) is the simplest carboxylic acid. Formate is an intermediate in normal metabolism. It is responsible for both metabolic acidosis and disrupting mitochondrial electron transport and energy production by inhibiting cytochrome oxidase activity, the terminal electron acceptor of the electron transport chain. Cell death from cytochrome oxidase inhibition by formate is believed to result partly from depletion of ATP, reducing energy concentrations so that essential cell functions cannot be maintained. Furthermore, inhibition of cytochrome oxidase by formate may also cause cell death by increased production of cytotoxic reactive oxygen species (ROS) secondary to the blockade of the electron transport chain.

Indoximod (NLG-8189) is a methylated tryptophan with immune checkpoint inhibitory activity. Indoximod inhibits the enzyme indoleamine 2, 3-dioxygenase (IDO), which degrades the essential amino acid tryptophan, and may increase or maintain tryptophan levels important to T cell function. Tryptophan depletion is associated with immunosuppression involving T cell arrest and anergy.

PZL-A, an activator of mtDNA synthesis, restored the function and activity of the most common POLγ mutant variant and activated mtDNA synthesis in the cells of pediatric patients with fatal diseases, thereby enhancing the oxidative phosphorylation mechanism and the biogenesis of cellular respiration, and can be used to treat progressive diseases associated with mtDNA depletion.

DX3-234 is a potent oxidative phosphorylation (OXPHOS) inhibitor that acts by inhibiting complex I in the mitochondrial electron transport chain (ETC), leading to intracellular ATP depletion and cell death, and can be used for the treatment of specific cancers dependent on aerobic metabolism, such as pancreatic cancer.

Teneliximab (BMS 224819) is a chimeric monoclonal antibody and a tumor necrosis factor receptor superfamily member 5 (CD40) inhibitor that blocks CD40-CD40L interactions.Teneliximab exerts its partial agonist activity through CD40 and peripheral B-cell depletion, and may be used to study organ transplant rejection and rheumatoid arthritis.

Dicoumarol (Dicumarol) is a hydroxycoumarin originally isolated from molding sweet-clover hay, with anticoagulant and vitamin K depletion activities. Dicoumarol is a competitive inhibitor of vitamin K epoxidereductase; thus, it inhibits vitamin K recycling and causes depletion of active vitamin K in blood. This prevents the formation of the active form of prothrombin and several other coagulant enzymes, and inhibits blood clotting.

Benralizumab (MEDI-563) is a monoclonal antibody targeting the interleukin-5 receptor alpha (IL-5Rα). It enhances antibody-dependent cell-mediated cytotoxicity, leading to a rapid depletion of eosinophils. Benralizumab is used for severe eosinophilic asthma and can be employed to prevent exacerbations of chronic obstructive pulmonary disease.

Palmitoylcarnitine chloride (Palmitoyl DL-carnitine chloride) is a mitochondrial fatty acid oxidation intermediate that mediates intralipid cardioprotection.Palmitoylcarnitine chloride eliminates colorectal cancer cell survival by depletion of glutathione. induces cancer cell death and regulates the interaction between protein kinase C βII and its receptor RACK1.

amyloid P-IN-1 can be used in studies about diseases with depletion of serum amyloid P components such as Alzheimer's disease, amyloidosis, osteoarthritis, and type 2 diabetes mellitus.

BHPI is a potent inhibitor of nuclear estrogen receptor ERα–regulated gene expression that induces sustained ERα-dependent activation of the endoplasmic reticulum stress sensor and unfolded protein response, leading to persistent inhibition of protein synthesis, and in ERα-positive cancer cells it hyperactivates plasma membrane PLCγ to generate IP3, deplete ER calcium stores via IP3R channels, and convert the normally protective UPR into a toxic response, making BHPI a valuable probe for estrogen signaling and ER stress–based cancer research.

GPP78 is a potent inhibitor of Nampt (IC50: 3.0 nM for nicotinamide adenine dinucleotide (NAD) depletion). GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells (IC50: 3.8 nM by inducing autophagy). GPP78 has anti-cancer and anti-inflammatory effect

PTC-028 selectively suppresses cancer cells whereas normal cells remain unaffected. PTC-028 is an orally bioavailable inhibitor of stem cell factor BMI-1 in ovarian cancer. The depletion of BMI-1 by PTC-028 causes caspase-mediated apoptosis.

Antibiofilm agent-12 (Compound C13), an antifungal belonging to the carbamate derivatives, exhibits significant antifungal activity against Candida auris, with an MIC90 of 237.9 μM. It inhibits the drug efflux pump activity of Candida auris and promotes ergosterol depletion, thereby hindering the formation of Candida auris biofilms and reducing its metabolic flexibility. Additionally, Antibiofilm agent-12 demonstrates antifungal efficacy in a C. elegans model following Candida auris infection.

4-Bromoamphetamine hydrochloride is an amphetamine derivative that functions as a serotonin-norepinephrine-dopamine releasing agent (SNDRA) and induces stimulant effects. It is highly neurotoxic and results in long-term serotonin depletion.

Ro4368554 is a selective 5-HT6 antagonist capable of crossing the blood-brain barrier. It can reverse memory deficits caused by scopolamine and tryptophan depletion. Ro4368554 is applicable for research related to memory impairments.