A natural alkaloid with antiviral properties, inhibiting the replication of hepatitis B alone and in combination with lamivudine; prevents fibrosis in a number of organs including liver, at least in part by interfering with TGF-β signaling.

A succinimide that is converted to N-desmethylmethosuximide, a channel blocker that targets low threshold calcium currents; inhibits CYP2C19-mediated metabolism of biguanides; has anticonvulsant properties in clinical trials.

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

A selective nonphosphoinositide inhibitor that specifically disrupts PIP3/Akt PH domain binding (IC50 = 31 μM); suppresses PI3K-PDK1-Akt-dependent phosphorylation, which reduces cell viability and induces apoptosis in PTEN-deficient U87MG glioblastoma cells (IC50 = 37 μM).

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

A selective β-adrenoceptor agonist that shows high affinity for β1, β2, and β3 (Ki = 224, 458, and 1,570 nM, respectively); inhibits contractions in isolated field stimulated rat vas deferens at low concentrations (EC₅₀ = 45.6 nM); increases cAMP levels and can…

A reversible inhibitor of serine proteases such as trypsin (Ki = 0.06 pM), chymotrypsin (Ki = 9.5 nM), and kallikrein (Ki = 0.8 nM); widely used as a protein purification tool to prevent proteases present in tissue samples from degrading the protein of interest.

An essential fatty acid and the most abundant ω-3 fatty acid in neural tissues, especially in the retina and brain; constitutes as much as 40% of the total PUFA pool in retinal and neuronal membranes; dietary supplementation via fish oil inhibits the progression of atherosclerosis and delays…

DETA NONOate is a NO donor. It spontaneously dissociates in a pH-dependent, first-order process with a half-life of 20 hours and 56 hours at 37°C and 22-25°C, pH 7.4, respectively, to liberate 2 moles of NO per mole of parent compound.

An irreversible, noncompetitive inhibitor of PARP1 that disrupts binding between PARP1 and DNA by interacting with the DNA binding domain; produces rapid apoptosis in the various cancer cell (IC50s = 40-128 μM).

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

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 cell-permeable, fluorescent probe for DNA that is useful as a marker of nuclei for cell cycle studies in combination with BrdU and to distinguish nuclear morphology in apoptotic cells.

The CysLTs, LTC4 and LTD4, are potent mediators of asthma and hypersensitivity. They induce bronchoconstriction, increase microvascular permeability, and are vasoconstrictors of coronary arteries. Their biological effects are transduced by a pair of GPCRs, CysLT1 and CysLT2. Montelukast (sodium…

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 synthetic cytokinin used as a media supplement to regulate growth in woody plant tissue cultures and micropropagations; concentrations below 1 µM promote axillary proliferation, whereas concentrations above 1 µM can stimulate the formation of callus, adventitious shoots, or somatic embryos.

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.

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

A competitive HDAC inhibitor that inhibits HDAC1 (IC50 = 0.25 μM) and HDAC3 (IC50 = 0.30 μM); causes cell differentiation, cell cycle arrest, or apoptosis.

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 dipyridinyl compound that demonstrates high in vitro and ex vivo selectivity for COX-2 over COX-1.

A minor alkaloid produced in plants of the Solanaceae family, including tobacco; detection in urine is used as an indicator of tobacco use; diminishes Aβ production, reduces the transcription and protein levels of β-secretase, and dose dependently inhibits NF-κB activation.

A cell permeable, competitive inhibitor of HIF-1α prolyl hydroxylase; stabilizes HIF-1α expression at normal oxygen tensions in cultured cells at concentrations between 0.1 and 1 mM.

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 potent dopamine receptor agonist that binds the D2 receptor with highest affinity (Ki = 2.5 nM); avidly binds the serotonin receptors 5-HT1A and 5-HT1D (Ki = 12.9 and 10.7 nM, respectively), as well as α and β adrenoreceptors.

An intermediate in the generation of adenine and methionine that is produced by the decarboxylation of SAM; a potent agonist of adenosine receptors (Kis = 0.15, 1.13, 13.9, and 0.68 μM for A1, A2A, A2B, and A3, respectively); inhibits several enzymes at higher concentrations.

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…

An endogenous CB neurotransmitter that binds to both CB1 and CB2 receptors.

An irreversible inhibitor of ornithine decarboxylase that suppresses polyamine biosynthesis; displays antiangiogenic, cytostatic, and antiparasitic effects.

A prodrug for mycophenolic acid, an inhibitor of inosine monophosphate dehydrogenase; blocks de novo GTP generation as well as RNA and DNA synthesis; inhibits lymphocyte proliferation and activation; used to benefit organ transplantation as well as autoimmunological diseases like lupus.

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