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.

CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.

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

Keystone essential fatty acid that is converted by COX, LO, and epoxygenase enzymes into more than 150 potent metabolites in species ranging from fungi to plants to mammals.

A β-lactam antibiotic in the cephalosporin class.

A non-protein amino acid that chelates iron and copper; inhibits certain enzymes that contain iron or copper, including arginase (IC₅₀ = 3.7 µM).

A potent inhibitor of both MEK 1 and 2 that works in an ATP-noncompetitive fashion (IC₅₀s = 0.7 and 0.9 nM, respectively); blocks dual phosphorylation of ERK1/2 and stops cell cycling in cancer cell lines, both in vitro and in multiple tumor models in mice.

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 potent, selective antagonist of the serotonin 5-HT6 receptor (pKi = 8.53); has been used in cells and in animals.

A naturally occurring agonist for the nuclear receptor Nur77 (IC₅₀ = 0.278 nM); induces apoptosis in cancer cells and retards xenograft tumor growth; induces genes related to gluconeogenesis and decreases atherosclerosis progression in mice fed a high fat/high cholesterol diet.

A synthetic H2S donor that can be readily esterified with other moieties, including therapeutics and targeting motifs; used both in cells and in animals for comparative studies with derived chimeras.

Hydroxy linoleins are a mixture of 132 possible isomers of mono-, di-, and tri-hydroxy compounds produced by the autoxidation of trilinolein and subsequent reduction of the hydroperoxides. Autoxidation of linoleic acid containing triglycerides (i.e., trilinolein) in vivo could result in the…

Palmitic acid ethyl ester is a neutral, lipid-soluble form of the free acid. It is one of the fatty acid ethyl esters that increase cytosolic Ca2+ concentration leading to pancreatic acinar cell injury due to excessive consumption of ethanol.

A-77-01 is a potent inhibitor of the TGF-β1 receptor ALK5 (IC₅₀ = 25 nM). It has no effects on BMP-regulated transcriptional activity or MAPK pathways. A-77-01 efficiently prevents the growth inhibitory effects of TGF-β on lung epithelial Mv1Lu cells. It completely blocks…

A mycotoxin produced by A. ochraceus, A. carbonarius, and P. verrucosum that is commonly found as a food contaminant (Tolerable Weekly Intake = 100 ng/kg body weight per day); triggers nephropathy, induces renal adenomas, and initiates skin tumors through events involving oxidative stress,…

Best known as a potent dual inhibitor of c-Src and Abl (IC50 = 1.2 and 1.0 nM, respectively); can be effective in regulating tumor growth and differentiation; also inhibits other members of the Src and TEC families and certain other kinases at nanomolar concentrations.

An inhibitor of Wnt production that impairs Wnt pathway activity (IC₅₀ = 27 nM in vitro) by inactivating Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins; used to suppress embryonic stem cell self-renewal and to decrease cancer cell proliferation,…

A DR5 agonist (Kd= 1.2 µM; IC₅₀ = 2 µM) that induces DR5 clustering, which leads to the initiation of FADD/caspase-8-dependent apoptosis in various cancer cells.

An analog of thalidomide that, at 10 μM, alters gene expression and cell viability in a range of cancer cell lines; induces proliferation and enhances the functional capacity of T-lymphocytes, amplifying co-stimulatory signaling pathways.

A nuclesoside analog that disrupts DNA synthesis in blood cells; effective in a number of animal tumor systems including LI210 leukemia, CD8F mammary adenocarcinoma, P388 leukemia, and human LX-1 lung tumor xenograft and displays anticancer activity against human hematological malignancies in vivo.

An internal standard for the quantification of PGE2-1-glyceryl ester by GC- or LC-MS.

A cell-impermeable, negatively charged tetrazolium dye that produces a water-soluble formazan when reduced at the cell surface by cellular-derived NADH and an electron mediator.

A microbial metabolite that binds the TCR on Vγ9Vδ2 peripheral blood lymphocytes with high affinity (EC50 = 0.39 nM); induces the expansion of human memory Vγ9Vδ2 T cells.

A potent and selective inhibitor of Wip1 (IC₅₀ = 6 nM); increases phosphorylation of Wip1 substrates and blocks cell cycling in cancer cells; orally bioavailable, causing inhibition of lymphoma xenograft growth in mice.

A fluorogenic substrate that can be cleaved specifically by group I caspases.

A metabolite produced during GCDH deficiency and used as a biomarker of glutaric acidemia type 1.

A selective inhibitor of 15-hydroxy PGDH (IC₅₀ = ~10 µM).

A potent and selective inhibitor of DGAT-1 (IC₅₀ = 19 nM); has high oral bioavailability (100%) in rats with a moderate half-life of 6.8 hours; significantly blocks an increase in plasma triglyceride levels following a corn oil bolus in rats.

A potent inhibitor of PI3K isoforms α, δ, and γ (IC₅₀s = 0.28, 0.12, and 0.97 nM, respectively) that is 31 times less potent at PI3Kβ; has increased potency in cancer cell lines harboring PIK3CA-activating alterations, and is effective in vivo.

A selective slow off-rate inhibitor of Raf kinases (IC₅₀s = 8.3, 2.4, and 1.4 nM for wild type B-Raf, mutant B-RafV600E, and c-Raf, respectively); shows significant antiproliferative activity against mutated BRAF or mutated NRAS cancer cell lines and xenograft models.

A hybrid molecule of indomethacin and an NO donor which combines the anti-inflammatory properties of an NSAID with the gastrointestinal protective effects of NO.

A common 16-carbon saturated fatty acid that represents 10-20% of the normal human dietary fat intake.