Aflatoxins are mycotoxins found in foods and livestock feeds that were initially produced by species of Aspergillus. Aflatoxin M1 is the hydroxylated metabolite of aflatoxin B1; it inhibits DNA synthesis and induces cell cycle arrest.

An inhibitor of β-catenin/Tcf-mediated transcription and an antagonist of ligand-dependent activation of PPARγ and PPARδ; blocks the recruitment of β-catenin and GRIP1 to PPARγ and PPARδ; selectively toxic to some carcinoma cell lines expressing the…

A broad-spectrum benzimidazole anthelmintic that is active against gastrointestinal parasites (IC₅₀ = 0.30 µM against Giardia in vitro) by targeting tubulin; activates HIF-1α, abrogating oxidative stress-induced death in primary neurons in vitro.

An analog of trimethoxy resveratrol; inhibits the growth of a variety of human tumor cell lines at concentrations form 0.4 to 2 µg/ml, which is 5-6 times more potent than resveratrol

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

A potent, selective inhibitor of ATR (IC₅₀ = 5 nM); inhibits the growth of LoVo colorectal adenocarcinoma cells in vitro and significantly reduces the growth of LoVo xenografts in mice.

A cell-permeable bis-indolo (indirubin) compound that acts as a highly potent, selective, reversible, and ATP-competitive inhibitor of GSK3α/β (IC₅₀ = 5 nM); inhibition of GSK activates the Wnt-signaling pathway and sustains pluripotency in human and mouse ESCs; maintains…

A variety of natural products from plant sources, particularly flavonoids, have long been observed to have antioxidant activity with potential benefits for human health. Antioxidant triterpenes are less common. Celastrol is a triterpenoid antioxidant compound isolated from the Chinese thunder god…

A specific inhibitor of N-linked glycoslylation that blocks the first step of glycoprotein synthesis and induces protein unfolding; impairs the function of several receptor tyrosine kinases, including EGFR, ErbB2, ErbB3, IGF-IR, and ALK; radiosensitizes glioma and pancreatic adenocarcinoma cells to…

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…

Mn(III)TBAP is a cell-permeable SOD mimic. At a concentration of 30 µM, it decreases the doubling time of SOD-null E. coli. by 2-fold.

Atriopeptin III is an analog of atrial natriuretic peptide (ANP) that exhibits vasodilatory/hypotensive and diuretic activities. In rat kidneys, atriopeptin III increases the diameter of constricted afferent arterioles, decreasing blood pressure.

An inhibitor of non-structural protein 5A of hepatitis C virus; effectively reduces or eliminates certain genotypes of hepatitis C virus in vivo, particularly when used in combination with other agents.

A non-lipid agonist of LPA2 (EC₅₀ = 0.10 µM) that is without effect at other LPA receptor subtypes; protects IEC-6 cells against caspase activation and apoptosis following irradiation; increases the survival of mice suffering from hematopoietic acute radiation syndrome after…

An orally active broad spectrum antifungal agent that blocks ergosterol biosynthesis by inhibiting the fungal CYP isoform CYP51; potently inhibits the mammalian analog CYP51A1 (IC₅₀ = 63.5 nM), as well as a variety of other CYP isoforms.

An inhibitor of SRE activation in PC3 cells (IC₅₀ = 6.4 μM), with 87% inhibition of SRE activation achieved at 100 μM; inhibits PC3 cell migration (IC₅₀ = 4.2 μM), as determined by a scratch wound assay; causes no cytotoxicity when evaluated by WST-1 assay.

A central component of energy storage and metabolism in vivo, providing the metabolic energy to drive metabolic pumps and serving as a coenzyme in a wide array of enzymatic reactions; acts a substrate for kinases involved in cell signaling and of adenylate cyclases that produce the second messenger cAMP.

A cell-permeable inhibitor that binds actin filaments, but not actin monomers, to inhibit polymerization at concentrations as low as 0.2 µM.

Misoprostol is a widely sold analog of PGE1 which has potent but relatively non-selective agonist activity with respect to the prostanoid EP receptor subgroup. Misoprostol has been used therapeutically for many years in humans for the treatment of gastric ulcer disease under the Searle tradename…

SC-560 is a member of the diaryl heterocycle class of COX inhibitors which includes celecoxib (Celebrex™) and rofecoxib (Vioxx™). However, unlike these selective COX-2 inhibitors, SC-560 is a selective inhibitor of COX-1. Using human recombinant enzymes, the IC₅₀ value for…

Reversibly inhibits dihyroorotate dehydrogenase, the rate-limiting step in the de novo synthesis of pyrimidines, preventing DNA synthesis of activated lymphocytes (IC₅₀s = 0.09, 3.5, and 12.5 μM for rat, mouse, and human, respectively); also inhibits tyrosine kinases responsible for…

A selective NMDA receptor antagonist (Kd = 1.4 μM) that competitively inhibits the glutamate binding site of NMDA receptors; widely used to study the activity of NMDA receptors particularly in regard to researching synaptic plasticity, learning, and memory.

An agonist of TGR5 (EC₅₀ = 0.82 µM); stimulates the secretion of GLP-1 in mice when given orally (30 mg/kg) after a glucose challenge, particularly when given with a DPP4 inhibitor; increases energy expenditure and reduces hepatic steatosis and adiposity in mice subjected to…

PGA2 is a naturally occurring prostaglandin in gorgonian corals where it may function in self defense. It is generally not present in mammals. PGA2 has low biological potency in most bioassays, but it does show some antiviral/antitumor activity. At a 25 µM concentration, PGA2 blocks the cell…

An oxidizing reagent that reacts with nitric oxide to form nitric dioxide and corresponding imino nitroxides.

The lipoxins are trihydroxy fatty acids containing a 7,9,11,13-conjugated tetraene. LXA4 was first described as a metabolite of 15-HpETE and/or 15-HETE when added in vitro to isolated human leukocytes. The material obtained in this manner consists of at least four distinct isomers: 5(S), 6(S);…

A selective inhibitor of RNA polymerase I-driven transcription of rRNA (IC₅₀s = 142, 113, and 54 nM in HCT116, A375, and MIA PaCa-2 tumor cells, respectively); demonstrates in vivo antitumor activity against human solid tumors in mouse xenograft models.

A methyl ester prodrug form of the NOS inhibitor L-NNA; exhibits Ki values of 15 nM, 39 nM, and 4.4 µM for nNOS (bovine), eNOS (human), and iNOS (mouse), respectively.

C-6 NBD ceramide is a biologically active fluorescent analog of short chain, membrane-permeable ceramides. It is as effective as C-6 ceramide in the inhibition of viral glycoprotein transport through the Golgi. C-6 NBD ceramide has been used as a fluorescent substrate for the activity of…

An inhibitor of NHE1, NHE2, and NHE3 (Kis = 0.02, 0.25, and 14 μM, respectively).

L-Arginine serves as a common substrate for both NOS and arginase in the cell. NOS catalyzes the oxidation of arginine to citrulline and NO with Nω-hydroxy-L-arginine (NOHA) formed as an intermediate. Arginase, on the other hand, catalyzes the hydrolysis of arginine into urea and L-ornithine.…

ALAL is a peptide sequence commonly used as a linker to conjugate compounds together to better target delivery of anticancer chemotherapeutics. Grade: ≥95%