A potent, selective inhibitor of BMP1 (IC₅₀ = 44 nM); effective in a cell-based model of collagen deposition is very effective at penetrating human skin in vitro.

A c-Myc inhibitor that binds to and distorts the bHLH-ZIP domain of c-Myc (Kd = 2.8 µM), thereby inhibiting c-Myc/Max heterodimer formation and inhibiting its transcriptional activity (IC₅₀ = 146 µM); cytotoxic to c-Myc-overexpressing cells lines (IC₅₀s = 15.6 and…

An A_2A adenosine receptor antagonist.

An anti-cancer natural product that acts on a variety of cellular pathways; activates caspases, inhibits anti-apoptotic proteins, alters expression of Bcl-2 and Bax; acts as a potent, slow inhibitor of Kir2.1 channels; inhibits the chymotrypsin activity of the 20S proteasome; has effects on AMPK,…

An anthelmintic antibiotic that at 0.001 µg/ml is fully effective at inhibiting growth in an H. contortus larval development assay.

A trisubstituted thiophene that selectively inhibits USP7 and the closely related USP47 (EC₅₀s = 4.2 and 4.3 μM, respectively); accelerates the degradation of the USP7 substrate HDM2 in several multiple myeloma cell lines (EC₅₀ =11 μM).

A macrocyclic antibiotic that exhibits cytotoxic effects in cancer cell lines, inhibiting cell proliferation (IC₅₀ = 221.3 nM in HL-60 cells); 1-4 μM inhibits oxidized LDL-induced accumulation of cholesteryl esters in macrophages; inhibits clathrin-coated pit-mediated endocytosis.

A selective, ATP-competitive inhibitor of CK2 with Ki values ranging from 0.5-1 µM.

A potent MAO inhibitor that preferentially targets MAO-A over MAO-B (Kis = 0.054 and 58 µM, respectively); also inhibits the sigma receptor σ1 on Jurkat human T lymphocyte cells (IC₅₀ = 31 nM).

A major Alternaria mycotoxins commonly found as a food contaminant (LD50 = 548 μg/egg in the chicken embryo toxicity assay) and linked to esophageal cancer in human populations at risk of high exposure; Mice fed 100 mg/kg/day orally for 10 months developed precancerous lesions on the esophageal mucosa.

A nonapeptide hormone primarily synthesized in the hypothalamus with roles in uterine contraction and lactation, social memory and attachment, sexual and maternal behavior, aggression, learning, anxiety, feeding, and pain perception.

A gold-thiol complex with anti-inflammatory and immunosuppressive actions; potently inhibits thioredoxin reductase (IC₅₀ = 0.2 μM); blocks LPS-mediated expression of inflammatory mediators at 10-20 μM and blocks NF-κB signaling; has applications in rheumatoid arthritis.

A bioactive metabolite of valproic acid that exhibits the same profile and potency of anticonvulsant activity in animal models as its parent compound without any observed teratogenicity and hepatotoxicity.

An antimitotic vinca alkaloid which irreversibly blocks mitosis by binding to tubulin (Ki = 85 nM) and inhibiting tubulin polymerization; exported from cells via the ABC transporter P-glycoprotein but not by Mrp1.

Inhibits PP1 (IC₅₀ = 1.7 μM) and PP2A (IC₅₀ = 0.2 μM) while only weakly inhibiting the activity of PP2B (IC₅₀ = 1 mM); stimulates cell cycle progression and induces premature mitosis and has been shown to be active in various cancer cell lines.

A full agonist of the serotonin 5-HT1A receptor and antagonist of 5-HT2A (Kis = 1 and 49 nM, respectively); also binds to dopamine D4 receptors (Kis = 4-24 nM); reduces 5-HT in the prefrontal cortex and dorsal raphe of conscious rats while increasing extracellular noradrenaline and dopamine.

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