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 colchicine derivative that inhibits tubulin polymerization (IC₅₀ = 2.1 μM) with low toxicity; suppresses microtubule dynamicity, inhibits cell migration, blocks microtubule assembly, and arrests cells in metaphase; used to synchronize cells and for karyotyping in cytogenetic studies.

A noncompetitive nicotinic acetylcholine receptor antagonist with preferential activity at the α3β4 subtype (IC₅₀ = 90-640 nM) compared to α4β2, α3β2, and α7 subtypes (IC₅₀s range from 1-7 μM).

PGE1 is the theoretical COX metabolite of DGLA, but it is virtually undetectable in the plasma of normal humans or other animals. Its pharmacology includes vasodilation, hypotension, and anti-platelet activities. The IC₅₀ of PGE1 for the inhibition of ADP-induced human platelet…

A protein cross-linking agent isolated from G. jasminoides Ellis; inhibits UCP2 activity; 5 µM genipin increases glucose-stimulated insulin secretion in isolated pancreatic islets chronically exposed to high levels of glucose; induces apoptosis in FaO rat hepatoma cells and human…

A sympathomimetic β2-adrenoceptor agonist that relaxes bronchial smooth muscle and at higher doses acts as an anabolic steroid, promoting skeletal muscle protein synthesis.

A glutamine analog that inhibits glutaminases (Ki = 6 µM) and other glutamine-utilizing enzymes, including cytidine triphosphate synthase.

A nitrogen mustard β-chloro-nitrosourea compound used as an alkylating agent to form interstrand crosslinks in DNA, which leads to cancer cell cytotoxity and apoptosis; also reported to inhibit glutathione reductase, thioredoxin reductase, and lipoamide dehydrogenase.

A potent uncoupler of oxidative phosphorylation in mitochondria that disrupts ATP synthesis by transporting protons across cell membranes.

An herbicide that is used to control a wide range of terrestrial and aquatic plants.

A cyclododecadepsipeptide potassium-selective ionophore antibotic; induces apoptosis in several cell tyes, including CHO cells, by stimulating potassium efflux.

A cell-permeable, stable free radical that is commonly used to evaluate the ability of compounds to act as free radical scavengers or hydrogen donors and to measure the antioxidant activity of tissue extracts; followed by color change from purple (absorbance at 515-528 nm) to yellow.

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.

An irreversible inhibitor of carnitine palmitoyltransferase 1, a mitochondrial enzyme involved in fatty acid β-oxidation (IC50 = 5-20 nM in rat liver); also acts as a direct agonist of PPARα.

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 benzothiazole derivative with anti-excitotoxic effects that acts by blocking the presynaptic release of glutamate, indirectly antagonizing glutamate receptors, and inactivating neuronal voltage-gated Na+ channels (ED50 = 2.3 μM); suppresses glutamate-induced seizures in rats (ED₅₀ =…

A selective non-peptide inhibitor of CXCR2, inhibiting IL-8 binding to CXCR2 (IC₅₀ = 22 nM).

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

A selective allosteric inhibitor of Bcr-Abl (IC₅₀s = 4.52, 0.38, and 0.93 µM against Bcr-Abl mutants G250E, E255V, and M351T, respectively); displays additive inhibitory activity against T315I Bcr-Abl mutants both in in vitro assays and in a recalcitrant T315I Bcr-Abl mutant mouse…

A selective α2-adrenergic receptor agonist (Ki = 183 nM) that lowers intraocular pressure by decreasing aqueous humor synthesis and increasing drainage through uveoscleral outflow; protects rat retinal ganglion cells against glutamate excitotoxicity by inhibiting glutamate release and…

A triazole, antifungal agent that inhibits a broad range of pathogenic yeasts, including Candida (MIC = 0.03-8 µg/ml), and filamentous fungi such as Aspergillus, Scedosporium, and Fusarium by disrupting ergosterol synthesis.

A second-generation antipsychotic designed to antagonize both D2 and 5-HT2A receptors with little effect on cholinergic and β-adrenergic receptors; affects α2-adrenergic and histamine H1 receptors.

A potent antagonist of dopamine receptors (IC₅₀s = 1.0 and 0.9 nM for D2 and D3, respectively);,also avidly binds α1- and α2-adrenergic receptors, histamine H1 receptor, and serotonin (5-HT) receptors 5-HT1D and 5-HT2A (Kis = 10, 80, 3.4, 19, 1.2 nM, respectively).

An HDAC inhibitor, antitumor agent that at 10 μM can induce oxidative stress contributing to apoptosis and differentiation in MCF-7 breast cancer cells; inhibits T. gondii tachyzoite propagation in human fibroblasts (EC₅₀ = 80 nM) and inhibits P. falciparum growth in human red blood…

An inhibitor of Nav, blocking human Nav1.2, Nav1.5, and Nav1.8 with IC₅₀ values of 10, 62, and 96 μM, respectively.

An inhibitor of EGF receptor kinase with an IC50 value of 460 µM in the human epidermoid carcinoma cell line A431.

A potent, clinically-useful immunosuppressant; binds to FK-506 binding protein 12 (Ki = 0.2 nM) to inhibit calcineurin; regulates NO neurotoxicity, neurotransmitter release, and regulation of Ca2+ release via the ryanodine and IP3 receptors.

A potent and selective inhibitor of type 3 PDEs, inhibiting recombinant PDE3A and PDE3B with IC₅₀ values of 0.45 and 1.0 μM, respectively; has positive inotropic (stimulates cardiac muscle contractions) and vasodilatory effects when administered in vivo.

A selective S1P1 receptor agonist in both human and mouse.

A constituent of the Chinese herb Artemisia identified as having anticoagulant, hypolipidemic, vasorelaxant, antioxidant, and anti-inflammatory actions in experimental models.

An acyclic nucleoside phosphonate that acts as a reverse transcriptase inhibitor; demonstrates antiviral activity against herpes viruses, hepatitis B virus, and HIV in animal and clinical models of infections.

An ATP-competitive B-Raf inhibitor (IC₅₀ = 10 nM; Kd = 2.4 nM) that inhibits cell proliferation both in B-Raf mutated and wild-type melanoma cell lines.