A selective serotonin reuptake inhibitor (Ki = 6.2 nM in rat hypothalamus) with comparatively little effect on noradrenaline reuptake (Ki = 1,100 nM); potentiates the pharmacological effects of serotonin and its precursor, 5-hydroxy tryptophan, in the CNS resulting in antidepressant effects.

A small molecule inhibitor of MDMX.

A cell-permeable inhibitor of PTPs (IC₅₀s = 0.09-1.7 µM) through oxidation of the catalytic cysteine residue; inhibits redox-sensitive CYP isoforms with IC₅₀ values less than 10 µM; inhibits the protein methyltransferases SETD8, SETD2, G9a, SMYD2, CARM1, and PRMT3…

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 =…

11-deoxy PGE2 is a stable, synthetic analog of PGE2. In contrast to PGE2 which has bronchodilation effects, 11-deoxy PGE2 is a powerful bronchoconstrictor and is 5 to 30 times more potent than PGF2α in the contraction of human respiratory tract smooth muscle in vitro.

A major inactive metabolite of clopidogrel that is used as a reference standard for quantitative analysis of clopidogrel metabolism.

A potent inhibitor of MELK (IC₅₀ = 0.41 nM); blocks the phosphorylation of MELK-specific substrates and reduces the ability of MCF-7 breast cancer cells to invade and form spheroids in Matrigel; suppresses the growth of xenograft tumors in mice.

Functions as a potent laxative by inducing chloride secretion in colonic mucosa and releasing acetylcholine, which stimulates contraction of intestinal smooth muscle; also demonstrates anti-tumor activity (ED50s = 1-13 µM), inducing apoptosis in various cancer cells.

A stable, potent analog of erbstatin; inhibits EGFR tyrosine kinase in vitro with an IC50 of 0.14 µg/ml; inhibits EGF-stimulated growth in NIH3T3 cells with an IC50 value of 0.5 µg/ml; delays onset of EGF-induced DNA synthesis.

A natural meroterpene that has retinol-like effects on gene expression and properties of the skin; has antioxidant and antibacterial actions; inhibits DNA polymerase and UDP-glucuronosyltransferase 2B7 (IC50 = 41 µM).

A potent anti-mitotic drug that is 100-fold more active than resveratrol at inhibiting the growth of human colon cancer Caco-2 cells; inhibits tubulin polymerization in a dose-dependent manner (IC₅₀ = 4 μM) and enzymes involved in the synthesis of the polyamines, putrescine, and spermidine.

An orally-available, highly selective inhibitor of B-RafV600E (IC₅₀ = 13 nM); less effective against wild type B-Raf (IC₅₀ = 160 nM) as well as several other kinases; induces cell cycle arrest and apoptosis in cells and xenografts expressing the mutant of B-Raf.

A protein cross-linking agent isolated from G. jasminoides Ellis; inhibits UCP2 activity; 5 µM genipin increases glucose-stimulated insulin secretion in isolated pancreatic islets chronically exposed to high levels of glucose; induces apoptosis in FaO rat hepatoma cells and human…

A homolog of DHEA, characterized by the addition of an (R)-β-methyl group at the terminal ethanolamine carbon.

A potent and selective CB1 receptor inverse agonist (Ki = 243 nM; EC50 = 195 nM); a 10 µM concentration results in 100% and 35% displacement of [3H]-CP-55,940 at the CB1 and CB2 receptors, respectively.

A derivative of PGF2β with increased water solubility.

9β-hydroxy stereoisomer of PGF2α; much less active than PGF2α in antifertility and bronchoconstrictor activities; exhibits bronchodilating activity in guinea pigs and cats and antagonizes the bronchoconstrictor activity of PGF2α.

A selective inhibitor of Δ6 desaturase (IC50 = 0.2 µM in a rat liver microsomal assay) that completely blocks the conversion of linoleic acid to AA; orally active in vivo, decreasing edema in the carrageenan paw edema model in mice.

An inhibitor of the HATs p300 and pCAF (IC50 = 7 and 5 μM, respectively) that also inhibits the HAT Gcn5; promotes neurogenesis and ex vivo expansion of human hematopoietic stem cells; induces apoptosis in several types of cancer cells and has anti-inflammatory actions.

CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.

The primary metabolite of PGE2 in plasma which is formed through the 15-hydroxy PGDH pathway.

An extract from A. lappa, a burdock plant traditionally used in Japanese Kampo medicine for its antioxidant, anti-inflammatory, antiproliferative, and antiviral activity.

A mixture of the potent and selective CB1 receptor antagonist SLV 319 (Ki = 7.8 nM) and its distomer, SLV 319 (+)-enantiomer.

A conjugate of biotin and lysine used for derivatization or conjugation to proteins and other molecules with a medium-chain length spacer; also used as an anterograde, retrograde, or intracellular neuroanatomical tracer that is fixable with aldehyde-based fixatives.

An imidazotetrazine that is converted to a compound capable of alkylating DNA, thus interfering with DNA replication and leading to cytotoxicity in proliferating cells; rapidly and completely absorbed from the gastrointestinal tract after oral administration and readily crosses the blood-brain barrier.

An active metabolite of proguanil, produced by CYP2C19; an inhibitor of dihydrofolate reductase (Kis = 0.3 and 1.5 nM for Plasmodium and human forms, respectively).

A reversible inhibitor of PAD4 (IC50 = 50 nM) that binds to the low-calcium form of the enzyme; blocks the citrullination of PAD4 target proteins in human neutrophils and inhibits the formation of NETs in both mouse and human neutrophils.

A potent, ATP-competitive inhibitor of ROCKs including p160ROCK (Ki = 140 nM) and ROCK-II (IC50 = 800 nM); also inhibits PRK2 with an IC50 value of 600 nM.

A selective agonist of α2-adrenoceptors (Ki = 1.08 nM vs. 1750 nM for α1-adrenoceptors) that has sedative, antinociceptive, analgesic, and hypothermic actions; additive or synergistic with fentanyl-type opioids in reducing pain; has anesthetic sparing properties.

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 angiotensin metabolite that functions as a type 1 angiotensin II receptor agonist whereupon it can control hydroelectrolyte balance and demonstrates vasodilatory and anti-inflammatory actions in opposition to various adverse effects of angiotensin II.

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