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

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).

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.

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…

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 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.

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.

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 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.

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 thio analog of the purine base guanine that incorporates into DNA during replication, inducing double-strand breaks that destabilize its structure and result in cytotoxicity; used as a chemotherapeutic for acute leukemia and other types of cancer, including BRCA2-mutated tumors.

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

Azaperone is a butyrophenone tranquilizer that exhibits sedative activity through the inhibition of a-adrenergic receptors. Azaperone also inhibits dopamine receptors and histamine receptors; it also may display antiemetic, antipsychotic, antihistaminergic, and anticholinergic activities.

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.

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.

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

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.

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 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 benzothiazole derivative with anti-excitotoxic effects that acts by blocking the presynaptic release of glutamate, indirectly antagonizing glutamate receptors, and inactivating neuronal voltage-gated Na+ channels (ED50 = 2.3 μM); suppresses glutamate-induced seizures in rats (ED₅₀ =…

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 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.

A polypeptide antibiotic effective against Gram-negative bacteria, including P. aeruginosa, A. baumannii, and K. pneumoniae.

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 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.

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).

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

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