A non-selective α-adrenergic receptor antagonist with pKi values of 8.5, 9, and 8.4 for human α1A, α1B, and α1D adrenoceptors, respectively; used to relax smooth muscles of the prostate in clinical studies designed to examine treatments that improve lower urinary tract…

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 fluorescent indicator of peroxynitrite formation; neither NO, superoxide, nor hydrogen peroxide alone appear to oxidize DCFH.

An inhibitor of DNA methyltransferases that reduces hypermethylation associated with certain diseases, including myelodysplastic syndromes (IC50s = 2.4 and 2.6 μM for in vitro anti-myeloma activity) and cancer (IC50s ~ 0.4 μM for inhibiting proliferation of various cancer cell lines).

2-(hydroxymethyl)-Pyrimidine is a synthetic intermediate useful for pharmaceutical synthesis.

An imidazobenzodiazepine derivative that competitively inhibits benzodiazepine binding to GABAA receptors (IC₅₀ = 2 nM); used to reverse sedation induced by benzodiazepine drugs and is effective in the treatment of benzodiazepine overdose or withdrawal.

A natural sesquiterpene that inhibits the proliferation of a wide range of tumors and enhances the effects of various chemotherapies; 10-40 µg/ml dose-dependently induces apoptosis and cell cycle arrest in the G2/M phase in HepG2 cells, upregulating Fas/FasL expression.

7-Piperazin-1-yl-thieno[2,3-c] pyridine (hydrochloride) is a synthetic intermediate useful for pharmaceutical synthesis.

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…

An anionic oligopeptide-based bola-amphiphile that contains a hexane moiety flanked by a glycylglycine group at each end, which creates distinct hydrophilic and hydrophobic regions.

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…

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.

5-Bromotetralone is a synthetic intermediate useful for pharmaceutical synthesis.

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 N-acylethanolamide that inhibits dietary-restriction-induced lifespan extension in wild type and TOR pathway mutant nematodes; also has anti-inflammatory properties, suppressing the expression of IL-6 and MCP-1 in 3T3-L1 adipocytes in response to lipopolysaccharide.

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.

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

Aprotinin is a single chain polypeptide (58 amino-acids) crosslinked by three disulfide bridges, showing competitive and reversible inhibiton of proteolytic and esterolytic activity. Aprotinin forms stable complexes with, and blocks the active sites of serine protease enzymes. It is found in bovine…

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.

An unsaturated fatty acid found in royal jelly produced from honeybees; demonstrates longevity-promoting effects in C. elegans, down regulates matrix metalloproteinases (MMPs) in rheumatoid arthritis, inhibits VEGF-induced angiogenesis in HUVECs, facilitates differentiation of neurons from neural…

A synthetic intermediate used in glycosylation reactions.

Inhibits CKII (IC50 range of 4-10 µM), Cdk7 (IC50 = ~20 µM), Cdk8 (IC50 = ~20 µM), and Cdk9 (IC50 = 3 µM); inhibits elongation during RNA polymerase II transcription; triggers p53-dependent apoptosis of human colon adenocarcinoma cells; inhibits trans-activated transcription…

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.

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.

N-Oleoyl glycine is a putative substrate for peptidyl glycine α-amidating enzyme in the biosynthesis of oleoyl amide.

An antibacterial and coccidiostat compound that shows selective toxicity for HMLER breast cancer stem cells (IC₅₀ = ~24 μM); 8 μM treatment of 4T1 and MCF-7-Ras breast cancer cell lines decreases cancer stem cell growth ~2-fold and ~3-fold, respectively; 5 mg/kg inhibits mammary…

A flavonoid compound that acts as a powerful antioxidant; inhibits TBARS formation with an IC50 value of 6.34 µM; blocks oxLDL uptake by U937-derived macrophages at 20 µM; demonstrates potent chemopreventative potential by binding JAK1/STAT3 to inhibit neoplastic transformation of…

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

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

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 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.

An intermediary prodrug of fluorouracil, the pyrimidine analog that inhibits thymidylate synthase selectively in tumor cells, interfering with DNA synthesis; one of two intermediary metabolites formed during metabolic conversion of the chemotherapeutic prodrug, capecitabine, to fluorouracil.