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.

A prodrug that is rapidly catabolized in vivo to 5-fluorouracil when administered by rapid injection; inhibits thymidylate synthase (EC₅₀ = 0.6 nM), interfering with DNA synthesis; used to treat various cancers, particularly metastases to the liver.

A chromogenic substrate that can be cleaved by cathepsin G (Km = 1.7 mM), subtilisins, chymotrypsin (Km = 60 µM), chymase (Km = 4 mM), and cyclophilin; used for inhibitor screening and kinetic analysis.

3-HPA is an analog of AM404, which is a selective inhibitor of carrier-mediated transport of AEA. 3-HPA is metabolized by both COX-1 and COX-2 and also selectively and irreversibly inhibits COX-2 with an IC50 value of 2 µM.

An orally active broad spectrum antifungal agent that blocks ergosterol biosynthesis by inhibiting the fungal CYP isoform CYP51; potently inhibits the mammalian analog CYP51A1 (IC₅₀ = 63.5 nM), as well as a variety of other CYP isoforms.

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 aminonucleoside antibiotic that blocks protein synthesis in both prokaryotes and eukaryotes by causing premature termination of nascent polypeptide chains; used in assays for peptide-bond formation and elongation and also often used as selective agent in cell culture systems.

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

A thiazide-like diuretic that targets the Na+-Cl- cotransporter responsible for salt reabsorption in the distal convoluted tubule of the kidney (IC₅₀ = 0.3 µM in rat); inhibits human carbonic anhydrase isoforms VII, XII, and XIII (Kis = 2.1, 5.4, and 15 nM, respectively).

An intermediate in the biosynthesis of NAD+ that has been used to enhance NAD biosynthesis and glucose-stimulated insulin secretion in Nampt+/- mice and high-fat diet-induced type 2 diabetes mice.

A selective and irreversible inhibitor of the gastric H+/K+ ATPase pump (IC₅₀ = 1.1 μM).

A nonfixable red fluorescent dye (excitation max: 586 nm; emission max: 605 nm) that can be used as a specific marker for astrocytes and an activity-dependent probe for monitoring regulated exocytosis.

An analog of adenosine monophosphate that has antiviral activity; converted by cellular enzymes to tenofovir diphosphate, an obligate chain terminator that inhibits the activity of HIV reverse transcriptase and HBV polymerase.

An intermediate in the interconversion of glucose and galactose.

A specific, cell-permeable inhibitor of S6K1 (IC₅₀ = 160 nM); does not inhibit S6K2, MSK, or RSK, or many other unrelated kinases, under conditions in which it inhibits S6K1 activity.

A small molecule radiosensitizer that has proven to be an effective and nontoxic immunochemical hypoxia marker for human squamous cell carcinomas of the cervix, head and neck.

A broad-spectrum nitrofuran antibiotic used against urinary tract infections and as therapy for acute diarrhea of bacterial origin; inhibits the survival and migration of cancer cells, suppressing tumor growth and metastasis in vivo, at least in part by inhibiting STAT3 (IC₅₀ = 10 µM).

A PDMP mixture containing D-threo (1R,2R) and L-threo (1S,2S) PDMP; reduces the synthesis of glucosylceramide increases cellular ceramide, and induces cell cycle arrest.

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 agonist of GPR81 (EC₅₀ = 16 µM) that is inactive against the related GPR109a (HCAR2) receptor; stimulates lipolysis (increased serum free fatty acids) in mice fed high fat chow for 10 weeks; blocks basal ghrelin secretion by primary gastric mucosal cells.

A steroid hormone produced in the cortex of the adrenal glands that binds to both glucocorticoid and mineralocorticoid receptors; also is the precursor to aldosterone synthesis.

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.

Chlorogenic acid is a phenolic natural product isolated from the leaves and fruits of dicotyledonous plants, including the coffee bean. Structurally, chlorogenic acid is the ester of caffeic acid with the 3-hydroxyl group of quinic acid. Chlorogenic acid is an important factor in plant metabolism.…

A synthetic H2S donor that can be readily esterified with other moieties, including therapeutics and targeting motifs; used both in cells and in animals for comparative studies with derived chimeras.

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

DGLA is a metabolite produced by chain elongation of the essential fatty acid γ-linolenic acid. Ethyl DGLA is an esterified version of the free acid which is less water soluble, but more ammenable for the formulation of DGLA-containing diets and dietary supplements. DGLA has been advanced as…

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…

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 elongation product of γ-linolenic acid (18:3), rapidly metabolized by fatty acid desaturases to produce arachidonic acid (20:4); metabolized through the cyclooxygenase pathway to produce 1-series prostaglandins; can reduce atopic dermatitis and atherosclerosis when added to the diet of mice.

A benzothiadiazide that acts as a potentiator of AMPA receptors, positively modulating its response to glutamic acid (EC₅₀ = 3.8 µM); also a negative modulator of GABAA receptors, reversibly inhibiting both evoked and spontaneous inhibitory postsynaptic currents (IC₅₀ =…

Can be formed by the dimerization of two molecules of α-trans-cinnamic acid; significantly blocks inflammatory pain while having little effect on neurogenic pain, as indicated by the formalin test in mice.

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.