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

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 potent, reversible, ATP-competitive, and selective inhibitor of the Src family of protein tyrosine kinases: p56lck (IC₅₀ = 4 nM), p59fynT (IC₅₀ = 5 nM), Hck (IC₅₀ = 5 nM).

A selective non-peptide inhibitor of CXCR2, inhibiting IL-8 binding to CXCR2 (IC₅₀ = 22 nM).

A polymethoxylated flavone that has been shown to enhance adipogenesis and lipolysis, to inhibit α-glucosidase and α-amylase activity, and to suppress the expression of genes associated with inflammation by regulating IκBα.

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).

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

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…

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).

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…

Myriocin is an amino fatty acid antibiotic derived from certain thermophylic fungi, in this case Mycelia sterilia. It is a potent immunosuppressant having 10- to 100-fold more activity than cyclosporin A. Myriocin is a potent inhibitor of serine palmitoyltransferase (Ki = 0.28 nM), the enzyme that…

A non-selective NSAID exhibiting IC50 values of 0.5 and 2.33 µM for human recombinant COX-1 and COX-2, respectively.

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

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

A cyanobacterial toxin that targets protein and glutathione synthesis in hepatocytes (IC50s = 1.3 and 2.4 µM, respectively), inhibits uridine monophosphate synthase complex activity (Ki = 10 µM), and induces DNA damage.

An orally active broad spectrum antifungal agent that blocks ergosterol biosynthesis by inhibiting the fungal CYP isoform CYP51; potently inhibits the mammalian analog CYP51A1 (IC₅₀ = 63.5 nM), as well as a variety of other CYP isoforms.

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).

Beraprost is an analog of prostacyclin in which the unstable enol-ether has been replaced by a benzofuran ether function. This modification increases the plasma half-life from 30 seconds to several hours, and permits the compound to be taken orally. Doses of 20-100 µg in humans, given 1 to 3…

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 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.

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.

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

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 selective allosteric inhibitor of Bcr-Abl (IC₅₀s = 4.52, 0.38, and 0.93 µM against Bcr-Abl mutants G250E, E255V, and M351T, respectively); displays additive inhibitory activity against T315I Bcr-Abl mutants both in in vitro assays and in a recalcitrant T315I Bcr-Abl mutant mouse…

A selective inhibitor of ABHD6 (IC₅₀ = 10 nM) with negligible activity against other serine hydrolases such as DAGLβ; used both as a probe to study ABHD6 and as a negative control for studies of DAGLβ.

A colchicine derivative that inhibits tubulin polymerization (IC₅₀ = 2.1 μM) with low toxicity; suppresses microtubule dynamicity, inhibits cell migration, blocks microtubule assembly, and arrests cells in metaphase; used to synchronize cells and for karyotyping in cytogenetic studies.

A small molecule inhibitor of tankyrase 1 and 2 (IC₅₀ = 11 and 4 nM, respectively); increases the protein levels of the axin-GSK3β complex and promotes the degradation of β-catenin; inhibits colony formation of APC-deficient colorectal cancer cells at 0.33 µM.

A natural fungal metabolite which reversibly interferes with protein trafficking and secretion mediated by the Golgi apparatus and endoplasmic reticulum; directly and reversibly inhibits Sec7 domain-containing GEFs which are necessary for Arf activation associated with vesicular transport (IC50 =…

PGE1 is the theoretical COX metabolite of DGLA, but it is virtually undetectable in the plasma of normal humans or other animals. Its pharmacology includes vasodilation, hypotension, and anti-platelet activities. The IC₅₀ of PGE1 for the inhibition of ADP-induced human platelet…