2-Hydroxymyristic acid is an inhibitor of protein myristoylation requiring about 0.5 mM concentration for full inhibition of acylation.

A long-acting, selective β2-adrenergic agonist with bronchodilator actions (EC₅₀ = 0.25 µM) that demonstrates 2,818-fold selectivity for β2-adrenergic receptors over β1-adrenergic receptors.

An irreversible inhibitor of ornithine decarboxylase that suppresses polyamine biosynthesis; displays antiangiogenic, cytostatic, and antiparasitic effects.

4-Pyrimidinecarboxaldehyde, dimethyl acetal is a synthetic intermediate useful for pharmaceutical synthesis.

A competitive antagonist of muscarinic receptors that potently blocks signaling through M1, M2, and M3 (Kis = 25, 125, and 10 nM, respectively), resulting in muscle relaxation.

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 DPP-4 (IC₅₀ = 3.5-34 nM); also inhibits DPP-8 and DPP-9 (Ki = 810 and 95 nM, respectively) but not DPP-2 or FAPα; blocks the degradation of several circulating peptides, including incretins; reduces fasting and postprandial glucose levels and decreases inflammatory…

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…

2-(hydroxymethyl)-Pyrimidine is a synthetic intermediate useful for pharmaceutical synthesis.

A broad-spectrum tetracycline antibiotic which has a particularly long half-life in serum; commonly used in the treatment of acne in older patients; also has both anti-inflammatory and neuroprotective actions.

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

A water soluble, irreversible, broad spectrum inhibitor of serine proteases, including trypsin, chymotrypsin, plasmin, thrombin, and kallikreins; also inhibits NADPH oxidase.

A natural alkaloid that acts as a selective and reversible α2-adrenergic receptor antagonist (Ki = 12 nM); also acts as a receptor antagonist at the serotonin 5-HT2B receptor (Ki = 14.3 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 derivative of fluphenazine that contains an alkylating chlorethylamine chain, which produces irreversible protein binding; a relatively selective, irreversible antagonist of D2 receptors both in vitro (IC₅₀ = 100 nM) and in vivo; irreversibly inhibits calmodulin at higher doses…

A potent PR and GR antagonist with Ki value of approximately 1 nM.

A selective β-adrenoceptor agonist that shows high affinity for β1, β2, and β3 (Ki = 224, 458, and 1,570 nM, respectively); inhibits contractions in isolated field stimulated rat vas deferens at low concentrations (EC₅₀ = 45.6 nM); increases cAMP levels and can…

A potent, stable, and selective agonist analog of AEA with a Ki value of 2.2 nM at the isolated rat CB1 receptor; 325 times more potent at the CB1 receptor compared with the CB2 receptor; induces hypothermia in mice with the same efficacy as AEA, in spite of its much higher affinity for the CB1…

An intermediate in several metabolic pathways, including glycolysis and gluconeogenesis.

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.

An intermediary prodrug of fluorouracil, the pyrimidine analog that inhibits thymidylate synthase selectively in tumor cells, interfering with DNA synthesis; one of two intermediary metabolites formed during metabolic conversion of the chemotherapeutic prodrug, capecitabine, to fluorouracil.

20-HETE is a major biologically active CYP450 metabolite of arachidonic acid in the kidney and liver. It regulates renal vascular and tubular functions as well as vascular tone in the cerebral circulation. HET0016 is an inhibitor of 20-HETE formation in human renal microsomes with an…

A non-nucleoside DNA methyltransferase inhibitor (IC₅₀ = 115 nM in vitro) that significantly reduces the methylation of genomic DNA in cells at 10 μM without detectable toxicity.

A long chain saturated fatty acid ethyl ester found in small quantities in liverwort, C. concium.

A compound used to attach biotin to primary amines, such as lysines on the surface of proteins, under alkaline conditions (pH~8-9).

An 18-carbon saturated fatty acid that is structurally similar to the phospholipid-derived N-acyl ethanolamines; inhibits heat-induced firing of nociceptive neurons in rat dorsal horn; induces transient calcium influx in native dorsal root ganglion (DRG) cells and in the PTX-sensitive, DRG-like…

A natural flavonol and potent antioxidant with anti-inflammatory actions; activator of sirtuin 1, inhibitor of the spleen tyrosine kinase SYK, and suppressor of CD36 gene expression.

A NSAID that inhibits COX-1 and -2 activity with IC₅₀ values of 17.4 and 13.1 µM, respectively.

An atypical antidepressant with diverse actions, most notably on the glutamatergic system; attenuates glutamate release and modulates the function of AMPAR; acts as an agonist of the µ-opioid receptor (EC₅₀s = 194 and 641 nM for human and mouse receptors, respectively).

A broad spectrum, orally available kinase inhibitor that targets primarily tyrosine kinases, including VEGFR and EGFR, with IC₅₀ values in the nanomolar range; also potently blocks non-receptor tyrosine kinases, including ABL, RET, and SRC, as well as several serine/threonine kinases.

A progesterone analog (i.e., a progestin); does not bind the ER, however, two of its A-ring metabolites can bind ER and possess weak estrogenic activity.

A potent inhibitor of iNOS (IC₅₀ = 0.20 μM), with over 1,000-fold selectivity compared to eNOS (IC₅₀ = 350 μM).