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 =…

An intermediate in the synthesis of cysteine that is produced from homocysteine and serine by the action of cystathionine-β-synthase; excess cystathionine in the urine is a hallmark of cystathioninuria.

A derivative of testosterone and ethisterone that binds androgen receptors and sex hormone-binding globulin causing a 3-fold increase in free testosterone; possesses weak androgenic effects and inhibits the production of gonadotropins.

A substrate for the synthesis of RNA during the transcription process and the synthesis of DNA during DNA replication; participates in G-protein-related signal transduction where it is converted to GDP through the action of GTPases.

A ceramide analog that contains a mixture of all four possible stereoisomers.

POL is a common triglyceride component in seed and vegetable oils including olive, sesame, soybean, canola, corn, hazelnut, and many others. POL is one of the standard triglyceride components used for the USP analysis of sesame oil for pharmaceutical applications.

The major active lignin in fruits of the burdock plant A. lappa that demonstrates potent antiviral, anti-inflammatory, and antiproliferative activity.

An analog of thalidomide that, at 10 μM, alters gene expression and cell viability in a range of cancer cell lines; induces proliferation and enhances the functional capacity of T-lymphocytes, amplifying co-stimulatory signaling pathways.

A natural intermediate in the pteridine pathway that can be produced naturally from 7-oxobiopterin or in vitro by the oxidation of pterin by xanthine oxidase.

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 cytotoxic, quinoline alkaloid that inhibits the DNA enzyme topoisomerase I (Top I) by binding the Top1-DNA cleavage complex and inducing DNA-strand breaks; has strong anti-tumor activity and induces DNA damage at concentrations as low as 51 nM in whole cells and 12 nM in isolated nuclei in in…

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

An aminoglycoside antibiotic that shows potent activity against a broad spectrum of bacteria.

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.

A prodrug that is metabolized in vivo to RNH-6270, a nonpeptide angiotensin II antagonist that potently inhibits angiotensin binding to the AT1 receptor (IC50 = 7.7 nM) without affecting binding to the AT2 receptor; reduces blood pressure.

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 side-chain substituted oxysterol derived from dietary cholesterol that inhibits the cleavage of SREBPs; has been implicated in a variety of metabolic events including cholesterol homeostasis and atherosclerosis as well as antitumor and immunomodulating activities.

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 non-protein amino acid that chelates iron and copper; inhibits certain enzymes that contain iron or copper, including arginase (IC₅₀ = 3.7 µM).

A cell permeable, competitive inhibitor of HIF-PH with effective concentrations in the low µM range.

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.

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.

Pargyline is an irreversible inhibitor of monoamine oxidase (MAO) that is used clinically to treat moderate hypertension. At 10 mg/kg iv, pargyline induces a moderate decrease of systolic blood pressure in unanaesthetized hypertensive rats but not normotensive WKR or Sprague-Daley rats. The…

Phytochemical from cruciferous vegetables that demonstrates anticancer and chemopreventative effects (10-30 µM) involving the induction of Phase 2 enzymes, promotion of apoptosis, induction of cell cycle arrest, inhibition of cell proliferation, and inhibition of histone deacetylases and DNA…

A substrate of cathepsin C that accumulates inside lysosomes causing lysosome degradation; 50 μM can inhibit the cathepsin-dependent activation of caspase-8.

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.

An anti-inflammatory steroid.

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.

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 natural triterpene which stimulates wound healing; induces cell cycle arrest and apoptosis in breast cancer cells (IC50 = 5.9 µM for MCF-7 cells); blocks angiogenesis in glioblastomas; down regulates BACE1 while increasing ADAM10 maturation in primary rat cortical neurons; protects against…

A prodrug for A-771726 that regulates T lymphocyte progression through the cell cycle by selectively inhibiting de novo pyrimidine synthesis; used to slow the disease progression of rheumatoid arthritis and as an immunosuppressive agent to prevent rejection of transplant allografts and xenografts.

A cell-impermeable, negatively charged tetrazolium dye that produces a water-soluble formazan when reduced at the cell surface by cellular-derived NADH and an electron mediator.