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.

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

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 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 cyclic polypeptide-containing anticancer antibiotic that binds to DNA and blocks transcription by interfering with RNA synthesis; ~10 nM promotes cell death in a variety of tumors.

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

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).

The primary active component of the heat and pain-eliciting lipid-soluble fraction of the Capsicum pepper and present in natural hot pepper extracts; elicits a sensation of burning pain by activation of TRPV1 on small, non-myelinated polymodal C-type nociceptive nerve fibers and has been widely…

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.

A DNA alkylating agents that induces DNA interstrand and intrastrand crosslinks, cytotoxicity, and apoptosis; inhibits the growth of PC-3 prostate cancer cells with IC₅₀ values of 0.074 or 0.77 μM for sequential dosing or single dosing, respectively.

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.

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 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.

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.

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 nitrogen mustard β-chloro-nitrosourea compound used as an alkylating agent to form interstrand crosslinks in DNA, which leads to cancer cell cytotoxity and apoptosis; also reported to inhibit glutathione reductase, thioredoxin reductase, and lipoamide dehydrogenase.

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 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+…

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 toxin produced by cyanobacteria that inhibits the catalytic activity of protein phosphatases PP1C, PP1γ, and PP2A with Ki values of 0.15, 0.24, and 0.018 nM, respectively.

An antibacterial and coccidiostat compound that shows selective toxicity for HMLER breast cancer stem cells (IC₅₀ = ~24 μM); 8 μM treatment of 4T1 and MCF-7-Ras breast cancer cell lines decreases cancer stem cell growth ~2-fold and ~3-fold, respectively; 5 mg/kg inhibits mammary…

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 tricyclic antidepressant that inhibits the reuptake of serotonin and norepinephrine and acts as an antagonist at histamine, serotonin, adrenergic, and muscarinic receptors with Ki values in the nanomolar range.

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

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 amino-amide anesthetic that binds to the intracellular portion of voltage-gated sodium channels and blocks sodium influx into nerve cells, preventing the generation of an action potential; inhibits the uptake of dopamine in striatal synaptosomes by 47% at 100 µM.

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.

(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.

An analog of 1,24-dihydroxy vitamin D3 which, when used in a 4 μg/g ointment, suppresses psoriasis; inhibits the growth of both normal and psoriatic human keratinocytes (IC50 ~ 10 nM) via the vitamin D receptor; suppresses the production of RANTES and IL-8 by human dermal fibroblasts.

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 alkaloid that inhibits the growth of mouse leukemia P388 cells (IC₅₀ = 1.8 μg/ml); binds to and stabilizes the topoisomerase I-DNA binary complex, leading to DNA breakage and cell death (IC₅₀ = 5.07-12.6 μM); selectively inhibits CYP1A1 and CYP1A2 (IC50 = ~6 μM for…

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