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.

An antiviral analog of guanosine, inhibiting the reverse transcriptase of HIV type 1 with an IC₅₀ value of 5.3 μM; blocks retroviral replication.

A metabolite of dimetridazole, the nitroimidazole-based antibacterial and anticoccidial agent suspected to be carcinogenic and mutagenic to humans.

A threonine and glycine catabolite that can be converted to methylglyoxal by amine oxidases; at 0.10-5 mM acts as a pro-oxidant inducing cell death in RINm5f pancreatic β-cells; used as a growth substrate for Pseudomonas.

A tertiary amine that complexes with, and stabilizes, Cu(I) to accelerate azide-alkyne cycloadditions, as used in click chemistry.

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

A potent, semi-synthetic LXR agonist derived from extracts of the mayapple; induces the expression of the ABCA1 reverse cholesterol transporter to increase the efflux of cholesterol from enterocytes and thus inhibits the overall absorption of cholesterol (ED50 = 1 nM).

L-Citrulline is a by product of NO formation from metabolism of L-arginine that exhibits tocolytic and antioxidative activities. L-Citrulline was originally found in watermelon. In isolated rat uteri, L-citrulline decreases uterine contractile force through stimulation of the NO-cGMP relaxant…

A non-selective, irreversible COX inhibitor with IC₅₀ values of 0.75 and 1.25 mM for ovine COX-1 and COX-2, respectively.

A competitive antagonist of S1P1 and S1P3 receptors (pKis = 7.86 and 5.93, respectively); inhibits S1P-induced migration of thyroid cancer cells, ovarian cancer cells, and neural stem cells.

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 synthetic intermediate useful for pharmaceutical synthesis.

A selective PAR2 agonist that stimulates cell proliferation, phosphatidylinositol hydrolysis, and calcium mobilization in in vitro functional assays (pEC₅₀s = 6.7, 5.9, and 6.6, respectively); elicits pronociceptive activity in vivo.

A potent peptide agonist of the GLP-1 receptor (Ki = 136 pM); stimulates glucose-induced insulin secretion in isolated rat islets and proinsulin expression in mouse insulinoma βTC-1 cells, supporting efficacy in type 2 diabetes; protects hippocampal neurons against glutamate-induced apoptosis.

β-Gal-NONOate is a nitric oxide (NO) donor which releases NO following activation by β-galactosidase. β-Gal-NONOate is stabile in aqueous solution at neutral and acidic pH for several hours, exhibits good water solubility, and is able to cross the cell membrane. Following enzymatic…

Selectively inhibits MEK1/2; potently inhibits growth and survival of human INA-6 multiple myeloma cells and cytokine-induced osteoclast differentiation (IC50s = 10 and 18.2 nM, respectively); 30 mg/kg reduced tumor growth significantly in mice bearing H929 MM xenografts.

Betamethasone is a glucocorticoid receptor agonist that exhibits anti-inflammatory, immunosuppressive, and anti-ulcerative activities. Betamethasone is clinically used to treat skin irritations such as psoriasis and to accelerate preterm fetal lung development.

A polysaccharide made of α-D-glucose units that constitutes about 20% of starch; acts as an indicator, turning blue in the presence of iodine, and has also been coupled to magnetic beads for the isolation and purification of maltose-binding protein fusion proteins.

A homolog of LOEA, characterized by the addition of an (S)-α-methyl group at the methylene carbon adjacent to the amide nitrogen.

A polysulfated disaccharide that is used as a reference standard for sucralfate.

A blue non-fluorescent dye that is used as an oxidation-reduction indicator in cell viability assays in a variety of cells; can be reduced to the highly red-fluorescent product resorufin (excitation: 530-540 nm; emission: 585-595 nm) and used as a quantifiable detection agent in enzyme activity or…

A benzoimidazole that potently inhibits human and rat recombinant mPGES-1 (IC₅₀ = 0.09 and 0.9 µM, respectively); dose-dependently blocks PGE2 synthesis in isolated cells and whole blood treated with LPS or IL-1β; dose-dependently reduces PGE2 synthesis and cell recruitment…

A dietary carotenoid present in the macula region of the eye; high dietary intake correlates with reduced risk of age-related macular degeneration.

A lipid peroxidation product; actively modifies histidine and lysine residues on proteins and causes protein cross-linking.

An activator of sGC that binds to a regulatory site, resulting in activation in an NO-independent manner (Kd = 3.2 nM); reduces hypertension, limits cardiomyocyte hypertrophy, protects against ischemia/reperfusion injury, and reduces morbidity and mortality in response to endotoxic shock.

A potent inhibitor of LSD1 (IC₅₀ = 0.02 µM) that less effectively inhibits MAO-A and MAO-B (IC₅₀s = 1.38 and 0.72 µM); blocks the expression of IE genes of HSV and hCMV in mammalian cells; represses HSV primary infection in mice and blocks HSV reactivation from…

A more lipid soluble derivative of Tafluprost, a very potent FP receptor agonist (Ki = 0.4 nM).

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 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.

A precursor to Vitamin K2 that is capable of both redox cycling and arylating nucleophilic substrates by Michael addition; used as an antihemorrhagic agent and to inhibit the proliferation of various cancer cells.

Valproic Acid, Sodium Salt is a branched chain fatty acid which is reported to enhance central GABAergic neurotransmission and inhibit Na+ channels. Sodium Valproate is reported to cause inositol depletion, activate the ERK pathway, inhibit GSK-3α and GSK-3β. Valproic Acid has been…

A potent, selective antagonist of the β2-adrenergic receptor (Ki = 0.7 nM for the β2 receptor, compared with 49.5 and 611 nM for β1 and β3 receptors, respectively); active in vivo and often used to evaluate the actions of adrenergic receptor agonists.