A selective NMDA receptor antagonist (Kd = 1.4 μM) that competitively inhibits the glutamate binding site of NMDA receptors; widely used to study the activity of NMDA receptors particularly in regard to researching synaptic plasticity, learning, and memory.

A cell-permeable substrate for aminopeptidase M and leucine aminopeptidase that was developed for intracellular analysis of protease activities.

A broad spectrum antibiotic that is in the β-lactam subclass known as carbapenems; effective against many Gram-negative and Gram-positive bacteria and is more effective against P. aeruginosa than other carbapenems; not effective against MSRA.

A form of PS that contains the abundant long-chain (16:0) palmitic acid inserted at the sn-1 and sn-2 positions; commonly used in the generation of liposomes and other types of artificial membranes.

A quinone derivative that inhibits red blood cell PLA2 with a Ki value of 130 µM.

Ebselen acts as a glutathione peroxidase mimic and is an excellent scavenger of peroxynitrite with a rate constant of 2 x 106 M−1s−1. The glutathione peroxidase-like activity of ebselen inhibits cyclooxygenase and lipoxygenases at micromolar concentrations.

A cell-permeable, stable free radical that is commonly used to evaluate the ability of compounds to act as free radical scavengers or hydrogen donors and to measure the antioxidant activity of tissue extracts; followed by color change from purple (absorbance at 515-528 nm) to yellow.

An inhibitor of HMG-CoA reductase (IC50 = 5 nM) that has been shown to be more effective than atorvastatin, simvastatin, or pravastatin in decreasing LDL cholesterol and increasing HDL cholesterol.

A potent and selective PPARγ ligand. It binds to the PPARγ ligand-binding domain with a Kd value of 43 nM.

An elongation product of γ-linolenic acid (18:3), rapidly metabolized by fatty acid desaturases to produce arachidonic acid (20:4); metabolized through the cyclooxygenase pathway to produce 1-series prostaglandins; can reduce atopic dermatitis and atherosclerosis when added to the diet of mice.

A natural benzoquinone which directly binds and inhibits XIAP (IC50 = 4.1 μM); blocks growth while activating caspases and promoting apoptosis in cancer cells expressing high levels of XIAP; prevents NF-κB activation by inhibiting IKK; protects against XIAP- and caspase-dependent inflammation.

A channel blocker that acts on several TRP channels, including TRPM2, TRPM8, and TRPC6 (IC₅₀ = 1.7, 3.8, and 2.3 μM, respectively); inhibits PLA2, blocking the release of arachidonic acid when given at 50 μM.

An aminonucleoside antibiotic that blocks protein synthesis in both prokaryotes and eukaryotes by causing premature termination of nascent polypeptide chains; used in assays for peptide-bond formation and elongation and also often used as selective agent in cell culture systems.

A natural triterpene which stimulates wound healing; induces cell cycle arrest and apoptosis in breast cancer cells (IC50 = 5.9 µM for MCF-7 cells); blocks angiogenesis in glioblastomas; down regulates BACE1 while increasing ADAM10 maturation in primary rat cortical neurons; protects against…

A required cofactor for many enzymes including all NOS isoforms.

An imidazotetrazine that is converted to a compound capable of alkylating DNA, thus interfering with DNA replication and leading to cytotoxicity in proliferating cells; rapidly and completely absorbed from the gastrointestinal tract after oral administration and readily crosses the blood-brain barrier.

A fluorescent probe that can react with ONOO-, HOCl, and H2O2 in a similar manner to CBA, yet is formulated for improved solubility.

An agonist of GPR81 (EC₅₀ = 16 µM) that is inactive against the related GPR109a (HCAR2) receptor; stimulates lipolysis (increased serum free fatty acids) in mice fed high fat chow for 10 weeks; blocks basal ghrelin secretion by primary gastric mucosal cells.

3-HPA is an analog of AM404, which is a selective inhibitor of carrier-mediated transport of AEA. 3-HPA is metabolized by both COX-1 and COX-2 and also selectively and irreversibly inhibits COX-2 with an IC50 value of 2 µM.

A widely-used non-specific inhibitor of cAMP and cGMP PDEs (IC₅₀ = 19, 50, 18, 13, 32, 7, and 50 μM for PDE1, PDE2, PDE3, PDE4, PDE5, PDE7, and PDE11, respectively).

Spermine NONOate is a NO donor. It spontaneously dissociates in a pH-dependent, first-order process with a half-life of 39 minutes and 230 minutes at 37°C and 22-25°C, respectively, (pH 7.4) to liberate 2 moles of NO per mole of parent compound.

Chlorogenic acid is a phenolic natural product isolated from the leaves and fruits of dicotyledonous plants, including the coffee bean. Structurally, chlorogenic acid is the ester of caffeic acid with the 3-hydroxyl group of quinic acid. Chlorogenic acid is an important factor in plant metabolism.…

A natural triterpenoid carboxylic acid that is known to have antioxidative, antimicrobial, anti-inflammatory, and anticancer activities; inhibits Na+/K+-ATPase activity (IC50 = 24.7 μM) and blocks NF-κB activation in various human cancer cells lines (10-100 μM), inhibiting cell…

Pargyline is an irreversible inhibitor of monoamine oxidase (MAO) that is used clinically to treat moderate hypertension. At 10 mg/kg iv, pargyline induces a moderate decrease of systolic blood pressure in unanaesthetized hypertensive rats but not normotensive WKR or Sprague-Daley rats. The…

A substrate of cathepsin C that accumulates inside lysosomes causing lysosome degradation; 50 μM can inhibit the cathepsin-dependent activation of caspase-8.

ALA is an essential fatty acid found in leafy green vegetables. ALA, as part of a low saturated fat diet, helps prevent cardiovascular disease. ALA decreases blood pressure, serum cholesterol levels, and platelet aggregation.

An α-hydroxy acid, overproduced in 2-hydroxyglutaric aciduria; mutations in IDH1 and IDH2 cause these enzymes to convert isocitrate to 2-hydroxyglutarate; competitively inhibits α-ketoglutarate-dependent dioxygenases, including lysine demethylases and DNA hydroxylases.

The major active lignin in fruits of the burdock plant A. lappa that demonstrates potent antiviral, anti-inflammatory, and antiproliferative activity.

A dihydropyridine used as an antihypertensive agent due to its ability to block L-type and T-type calcium channels; also binds to adenosine A₁, A_2A, and A₃ receptors with K_i values of 8.96, 23.0, and 8.3 µM, respectively.

The oxidized form of NADPH; serves as a cofactor in various biological reactions.

Inhibits microtubule polymerization (IC₅₀ =3.2 μM) by binding to tubulin, which disrupts spindle formation during mitosis; blocks the growth of MCF-7 human breast carcinoma cells (IC₅₀ = 13 nM); inhibits neutrophil motility and activity (5 μmol/kg in a mouse model of…

An angiotensin II receptor blocker with a high affinity for the AT1 receptor (Ki = 2.7 nM) and exceptionally high bioavailability (60-80%); an insurmountable antagonist of AT1; act as a cardiovascular protective agent by effectively reducing blood pressure; also useful in treating diabetes and…