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 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).

A potent, selective antagonist of TRPV4 channels, blocking the influx of calcium induced by the TRPV4 agonist GSK634775 with IC₅₀ values of 2, 5, and 40 nM for rat, mouse, and human isoforms, respectively; effective in vivo, as it resolves pulmonary edema resulting from myocardial…

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 neuroexcitatory amino acid that functions as a NMDA and metabotropic glutamate receptor agonist; used to induce brain lesions in animal models of cognitive dysfunction.

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 natural fungal metabolite which reversibly interferes with protein trafficking and secretion mediated by the Golgi apparatus and endoplasmic reticulum; directly and reversibly inhibits Sec7 domain-containing GEFs which are necessary for Arf activation associated with vesicular transport (IC50 =…

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

A selective inhibitor of ABHD6 (IC₅₀ = 10 nM) with negligible activity against other serine hydrolases such as DAGLβ; used both as a probe to study ABHD6 and as a negative control for studies of DAGLβ.

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.

A small molecule inhibitor of tankyrase 1 and 2 (IC₅₀ = 11 and 4 nM, respectively); increases the protein levels of the axin-GSK3β complex and promotes the degradation of β-catenin; inhibits colony formation of APC-deficient colorectal cancer cells at 0.33 µM.

A potent, reversible, ATP-competitive, and selective inhibitor of the Src family of protein tyrosine kinases: p56lck (IC₅₀ = 4 nM), p59fynT (IC₅₀ = 5 nM), Hck (IC₅₀ = 5 nM).

A polymethoxylated flavone that has been shown to enhance adipogenesis and lipolysis, to inhibit α-glucosidase and α-amylase activity, and to suppress the expression of genes associated with inflammation by regulating IκBα.

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

Myriocin is an amino fatty acid antibiotic derived from certain thermophylic fungi, in this case Mycelia sterilia. It is a potent immunosuppressant having 10- to 100-fold more activity than cyclosporin A. Myriocin is a potent inhibitor of serine palmitoyltransferase (Ki = 0.28 nM), the enzyme that…

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.

An antibiotic that inhibits complex III of the mitochondrial ETC, preventing electron transport between cytochromes b and c, which results in the production of superoxide and eventual cell death; inhibits Bcl-2 and Bcl-xL proteins, inducing apoptosis.

An anti-coagulant; differs from (−)-warfarin by being five times less potent as a vitamin K antagonist; has a longer terminal elimination half-life (35-58 hours) than (−)-warfarin (24-33 hours).

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).

A natural chemical found in fresh ginger that activates TRPV1 (EC50 = 3.3 µM) as well as the TRP ankyrin receptor TRPA1 (EC50 = 10.4 µM).

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 selective EP1 antagonist that displays analgesic activity in mice (ED50 = 6.3 mg/kg when given subcutaneously) and in rats; inhibits the growth of glioma cell lines in vitro (IC50 = ~1 μM) and slows tumor growth in vivo; attenuates neuronal cell death in response to oxidative stress.

A selective S1P1 receptor agonist in both human and mouse.

A PAR4 antagonist (IC₅₀ = 140 nM) that exhibits 71-fold selectivity for PAR4 over PAR1 (IC₅₀ = 10 μM) in isolated human platelets.

A plant-derived steroidal triterpene that induces cell cycle arrest or apoptosis in a range of cancer cell lines; inhibits the growth of several breast cancer cell lines (IC₅₀s = 18-50 nM); suppresses the growth of tumors developed from MDA-MB-231 and 4T-1 breast cancer cells in mice.

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

An anticoagulant; differs from (+)-warfarin by being five times more potent as a vitamin K antagonist; has a shorter terminal elimination half-life (24-33 hours) than (+)-warfarin (35-58 hours).