An antifungal agent that acts as an inverse agonist to disrupt Hh signaling (IC₅₀ = 0.8 μM); treatment at 100 mg/kg twice per day has been shown to suppress the growth of medulloblastomas from a Ptch+/-p53-/- mouse allograft model.

An analog of β-D-glucose in which sulfur replaces the hydroxyl group at the one position, allowing diverse chemical reactions, including click chemistry and polymerization; can be labeled with technetium-99m for analytical and diagnostic procedures.

Nicotinic acetylcholine receptor agonist isolated from Nicotiana tabacum and Nicotiana rustica. Nicotine Tartrate finds an application as the nicotine active in a wide range of smoking cessation products such as nicotine lozenges and nicotine sub-lingual tablets. (-)-Nicotine ditartrate is a…

β-estradiol is a potent mammalian estrogenic hormone produced by the ovary. Triggers the production of gonadotropins leading to ovulation. β-Estradiol is used to study cell differentiation and transformations (tumorigenicity). The pharmacology and HPLC determination of β-Estradiol…

A metabolically stable adenosine analog that binds to adenosine A1, A2A, and A3 receptors with Ki values of 300, 80, and 1,900 nM, respectively; anticonvulsive activity in a rat model of generalized seizures.

A DNA alkylating agents that induces DNA interstrand and intrastrand crosslinks, cytotoxicity, and apoptosis; inhibits the growth of PC-3 prostate cancer cells with IC₅₀ values of 0.074 or 0.77 μM for sequential dosing or single dosing, respectively.

A catatoxic steroid that acts as an agonist of the rodent PXR at µM concentrations; mediates induction of hepatic CYP3A, Oatp2, and Cyp7a1, regulating both xenobiotic and bile acid homeostasis.

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 widely-used non-specific inhibitor of cAMP and cGMP PDEs (IC₅₀ = 19, 50, 18, 13, 32, 7, and 50 μM for PDE1, PDE2, PDE3, PDE4, PDE5, PDE7, and PDE11, respectively).

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

Adefovir is an antiviral prodrug that displays immunomodulatory activity. Adefovir is an acyclonucleotide analog that inhibits viral DNA polymerase, acting as a DNA chain terminator. Adefovir is primarily used to treat hepatitis B infection, but also displays activity against retroviruses. Adefovir…

An analog of folic acid and aminopterin that is used in the treatment of cancer, autoimmune diseases, ectopic pregnancy, and for the induction of medical abortions; induces adenosine release, inhibits the metabolism of folic acid, and blocks key enzymes in the synthesis of purines and pyrimidines…

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 calcium sensitizer that causes increased cardiac contractility by binding troponin C (EC₅₀ = 9 nM), promotes vasodilation by activating ATP-sensitive potassium channels on vascular smooth muscle cells (EC₅₀ = 0.28 µM), and performs a cardioprotective function by…

A synthetic intermediate used in glycosylation reactions.

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 synthetic intermediate useful for pharmaceutical synthesis.

A semisynthetic analog of taxol that inhibits microtubule disassembly (IC50 = 0.2 μM) and inhibits cell replication (IC50 = 0.13 μM); has applications in breast cancer and hormone-refractory prostate cancer; intended for research applications.

A fluorogenic substrate of β-glucuronidase that upon cleavage yields a blue fluorescent end product that can be monitored by UV light; typically used in the GUS reporter system for fluorescent detection of β-glucuronidase gene expression in E. coli and transformed plants.

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 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).

A natural retinoid that associates with CRBP-I and CRBP-II (Kds = 50 and 90 nM, respectively), which are involved in the intracellular transport of retinol; an intermediate of the phototransduction pathway of photoreceptors; can form toxic conjugates with proteins and lipids, leading to…

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 anti-inflammatory steroid.

An antipsychotic compound that displays high affinity for dopamine receptors (Kis = 2.4, 0.2, and 1.8 nM for D2, D3, and D4, respectively); also has actions as an antagonist, inverse agonist, or channel blocker, with lower affinities, at other receptors and channels.

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

A cell-permeable substrate for aminopeptidase M and leucine aminopeptidase that was developed for intracellular analysis of protease activities.

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.

ALA is an essential fatty acid found in leafy green vegetables. ALA, as part of a low saturated fat diet, helps prevent cardiovascular disease. ALA decreases blood pressure, serum cholesterol levels, and platelet aggregation.

A secondary metabolite produced by some species of lichen that binds FAS-II enzymes to produce antibacterial and antiplasmodial effects; inhibits PfFabZ and PfFabI (IC₅₀ = 10.7 and 36.1 µM, respectively) but shows low efficacy against the malaria parasite P. berghei…

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 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.