A potent and selective AhR antagonist (Ki = 1.2 nM).

An imidazoquinoline compound that activates TLR7 (EC₅₀ = 2.1 µM) on immune cells, inducing the production of IFN-α, IL-12, and other mediators; up-regulates the OGF receptor on cancer cells, blocking cell proliferation (IC₅₀ = 2 µM).

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.

Activates the aryl hydrocarbon receptor (Ki = 5.4 µM), inducing the expression of both detoxifying enzymes, resulting in pyocyanin degradation, and cytokines that facilitate the clearance of bacteria; accelerates neutrophil apoptosis, resulting in resolution of acute inflammation.

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 naturally-occurring dimethyl ether analog of resveratrol; acts as a powerful antioxidant, suppresses the synthesis of PGE2 from LPS-stimulated human peripheral blood mononuclear cells (IC₅₀ = 1.0 μM), and inhibits cell proliferation (IC₅₀ = ~60 μM); evokes effects that…

An ATP-competitive Pim-1 kinase inhibitor (IC₅₀ = 50 nM) that displays selectivity over the related kinases, Pim-2 and MEK1/2 (IC₅₀s = >20 µM).

A powerful effector in both the TetR and revTetR transcriptional regulator systems, binding the Tet repressor 35-fold more strongly than Tet; does not act a general inhibitor of translation and is a poor antibiotic.

MAHMA NONOate is a NO donor. It spontaneously dissociates in a pH-dependent, first-order process with a half-life of 1 minute and 3 minutes at 37°C and 22-25°C, respectively, (pH 7.4) to liberate 2 moles of NO per mole of parent compound.

A member of the 2-aryl propionic acid group of NSAIDs that reduces inflammation through inhibition of NF-κB and AP-1 activation; decreases survival of prostate tumor cells by inducing p75NTR protein expression; inhibits the enzyme γ-secretase thereby preventing the formation of the…

A potent disruptor of microtubules used as a chemotherapeutic compound; inhibits growth of cervical (HeLa), lung (A549), breast (MCF-7), colon (HT-29), ovarian (OVG-1), and pancreatic (PC-Sh) carcinomas with IC50 values ranging from 2.5-7.5 nM; induces mitotic arrest and initiates apoptosis of…

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

A synthetic cytokinin used as a media supplement to regulate growth in woody plant tissue cultures and micropropagations; concentrations below 1 µM promote axillary proliferation, whereas concentrations above 1 µM can stimulate the formation of callus, adventitious shoots, or somatic embryos.

A succinimide that is converted to N-desmethylmethosuximide, a channel blocker that targets low threshold calcium currents; inhibits CYP2C19-mediated metabolism of biguanides; has anticonvulsant properties in clinical trials.

An abundant oligosaccharide in the milk of many mammals, including cows and humans, particularly postpartum; avidly binds several viral strains, including strains of influenza, HIV-1, reovirus, and polyomavirus, in some cases altering viral infectivity.

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…

A glucosamine-nitrosourea which is commonly used to induce experimental diabetes in animals; specifically targets beta cells, entering via the glucose transporter GLUT2 and causing alkylation of DNA, leading to the destruction of beta cells.

An organic polysulfide compound found in garlic that acts as an H2S donor; reduces the survival of prostate cancer PC-3 cells (IC50 = 22 μM) and inhibits the growth of human colon adenocarcinoma HCT15 cells (IC50 = 11.5 μM); suppresses the growth of PC-3 xenografts in vivo in mice and induces…

An intermediate in the catabolism of aromatic amino acids; formed in excess during alkaptonuria.

A channel blocker that acts on several TRP channels, including TRPM2, TRPM8, and TRPC6 (IC₅₀ = 1.7, 3.8, and 2.3 μM, respectively); inhibits PLA2, blocking the release of arachidonic acid when given at 50 μM.

An anti-inflammatory compound from the diaryl heterocycle class that selectively inhibits COX-2 (IC50s = 22.9 and 0.05 μM for COX-1 and COX-2, respectively; displays chemopreventive activity in multiple tumor types via proapoptotic effects independent of its capacity to block COX-2.

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 dopamine receptor agonist that binds the D2 receptor with highest affinity (Ki = 2.5 nM); avidly binds the serotonin receptors 5-HT1A and 5-HT1D (Ki = 12.9 and 10.7 nM, respectively), as well as α and β adrenoreceptors.

A selective NMDA receptor antagonist (Kd = 1.4 μM) that competitively inhibits the glutamate binding site of NMDA receptors; widely used to study the activity of NMDA receptors particularly in regard to researching synaptic plasticity, learning, and memory.

An endogenous CB neurotransmitter that binds to both CB1 and CB2 receptors.

A potent inhibitor of PDE5 (IC50 = 1-5 nM) that also blocks the activity of PDE11 (IC50 = 10-33 nM); IC50 values against other isoforms of PDE are in the micromolar range; pharmacokinetics are highlighted by its prolonged duration of effect.

An analog of trimethoxy resveratrol; inhibits the growth of a variety of human tumor cell lines at concentrations form 0.4 to 2 µg/ml, which is 5-6 times more potent than resveratrol

A cell-permeable, potent inhibitor of both SHP-1 and SHP-2 (IC₅₀ = 355 and 318 nM, respectively); much less effective against other protein tyrosine phosphatases and DUSP26.

The reduced form of the electron acceptor NADP+ and acts as an electron donor in various biological reactions.

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 “hybrid” analog which incorporates components of both the AEA-like and dopaminergic neurotransmitter pathways; is nearly inactive as a TRPV1 ligand and fails to elicit hyperalgesic or nocifensive responses in vivo; exhibits an “entourage” effect at concentrations of 0.1-10…

Carboxy-PTIO is a NO scavenger. It reacts stoichiometrically with NO and can be used for EPR detection of NO.