A glutamine analog that inhibits glutaminases (Ki = 6 µM) and other glutamine-utilizing enzymes, including cytidine triphosphate synthase.

An agonist of α2 adrenergic receptors (Ki = 194 nM); used for sedation, anesthesia, and analgesia in non-human mammals.

An intermediate produced from vitamin D2 by cytochrome P450 isoforms in vertebrates; subsequently metabolized to 1,25-dihydroxy vitamin D2, which is an agonist for the vitamin D receptor.

A macrolide that causes the formation of bundles of intracellular microtubules in non-mitotic cells, induces the formation of hyperstable tubulin polymers, and arrests cell cycling in mitosis; induces mitotic arrest at nanomolar IC50 values in cell lines from ovarian, breast, lung, colon, prostate,…

An herbicide that is used to control a wide range of terrestrial and aquatic plants.

An irreversible inhibitor of carnitine palmitoyltransferase 1, a mitochondrial enzyme involved in fatty acid β-oxidation (IC50 = 5-20 nM in rat liver); also acts as a direct agonist of PPARα.

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 indole diterpene which potently and reversibly inhibits large conductance Ca2+-activated K+ (BKCa) channels, as shown in patch clamp (Ki = 1.9 nM) and whole smooth muscle cell studies (Ki = 35.7 nM).

A prodrug for A-771726 that regulates T lymphocyte progression through the cell cycle by selectively inhibiting de novo pyrimidine synthesis; used to slow the disease progression of rheumatoid arthritis and as an immunosuppressive agent to prevent rejection of transplant allografts and xenografts.

A synthetic prodrug which is converted to the vitamin D receptor agonist 1,25-dihydroxy vitamin D3 in vivo; suppresses the synthesis and secretion of parathyroid hormone in secondary hyperparathyroidism; supports bone growth; provides renal and cardiovascular protection during chronic kidney disease.

Produced in fungi, including yeast, and invertebrates from ergosterol in response to ultraviolet radiation; metabolized first to 25-hydroxyvitamin D2 and subsequently to the active 1,25-dihydroxyvitamin D2.

A classical inhibitor of complex I of the mitochondrial electron transport chain, inhibiting NADH/DB oxidoreductase and NADH oxidase with IC₅₀ values of 28.8 and 5.1 nM, respectively; used in animal models of Parkinson’s disease.

A cyclododecadepsipeptide potassium-selective ionophore antibotic; induces apoptosis in several cell tyes, including CHO cells, by stimulating potassium efflux.

A neuroexcitatory amino acid that functions as a NMDA and metabotropic glutamate receptor agonist; used to induce brain lesions in animal models of cognitive dysfunction.

A CYP2C9 metabolite of the NSAID diclofenac that demonstrates anti-inflammatory and analgesic properties by inhibiting COX and suppressing PGE2 synthesis.

A hepatotoxic monocylic pentapeptide that acts as a potent inhibitor of protein phosphatase types 1 (PP1) and 2A (PP2A), exhibiting IC50 values of 1.8 and 0.026 nM, respectively.

An NSAID commonly used in animals to combat pain and inflammation, particularly as associated with osteoarthritis; inhibits both COX-1 and COX-2 (IC₅₀s = 22.3 and 3.9 µM, respectively) and also FAAH (IC₅₀ = 74 µM).

A neurotoxin that binds to voltage-gated sodium channels (IC₅₀ = 15 nM) on neurons at the neuromuscular junction, causing the channel to open irreversibly at potentials more negative than normal, discharging action potentials repetitively; ichthyotoxic at nanomolar concentrations.

An analog of wortmannin; irreversibly binds PI3K; inhibits recombinant PI3K and mTOR (IC₅₀ = 2.7 and 193 nM, respectively) and prevents the growth of LNCap cells (IC₅₀ = 1.46 μM).

A pyrimadine analog that irreversibly inhibits thymidylate synthase, blocking the synthesis of thymidine which is required for DNA synthesis; widely used to treat many gastrointestinal tract adenocarcinomas.

Intended for use as an internal standard for the quantification of diclofenac by GC- or LC-MS.

A natural type B trichothecene produced by certain species of the fungus Fusarium; inhibits protein biosynthesis, binds to peptidyl transferase, and inhibits the synthesis of RNA and DNA; passes the blood-brain barrier at different rates in different animals.

A central nervous system modulator that is used to experimentally induce seizures in animals; used extensively to screen for compounds that block the production of nonconvulsive (absence or myoclonic) seizures.

A non-selective COX inhibitor with IC₅₀ values for ovine COX-1 and -2 of 0.1 and 6 µM, respectively; IC₅₀ values for human recombinant COX-1 and -2 are 1.67 and 24.6 µM, respectively.

Capsaicin is the primary active component of the heat and pain-eliciting lipid-soluble fraction of the Capsicum pepper. Capsaicin is present in natural hot pepper extracts along with a number of impurities, including dihydrocapsaicin and several lesser impurities. Separation by HPLC is required in…

(S)-Naproxen is a non-selective COX inhibitor. The IC₅₀ values for human recombinant COX-1 and -2 are 0.6-4.8 µM and 2.0-28.4 µM, respectively.

A dihydropyridine L-type calcium channel antagonist that displays antihypertensive and antianginal activity; selectively inhibits adenosine A3 receptors (Ki = 3.25 µM) and CYP3A4 catalytic activity (IC₅₀ = 0.148 µM); activates TRPA1 channels, producing an increase in Ca2+…

A potent, selective antagonist of TRPV4 channels, blocking the influx of calcium induced by the TRPV4 agonist GSK634775 with IC₅₀ values of 2, 5, and 40 nM for rat, mouse, and human isoforms, respectively; effective in vivo, as it resolves pulmonary edema resulting from myocardial…

A noncompetitive nicotinic acetylcholine receptor antagonist with preferential activity at the α3β4 subtype (IC₅₀ = 90-640 nM) compared to α4β2, α3β2, and α7 subtypes (IC₅₀s range from 1-7 μM).

An intermediate in the pathway leading to the production of 1,25-dihydroxy vitamin D3; plasma or serum levels are commonly used as an indicator of an individual’s vitamin D status.

A dihydropyridine L-type calcium channel blocker that selectively inhibits calcium influx in cardiac and vascular smooth muscle; inhibits calcium-induced contractions in depolarized rat aorta (IC₅₀ = 1.9 nM), displaying a slow rate of association and dissociation in isolated vascular and…

A potent uncoupler of oxidative phosphorylation in mitochondria that disrupts ATP synthesis by transporting protons across cell membranes.