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 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 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…

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.

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.

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 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 selective inhibitor of PI3Kγ

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.

The major metabolite of the gastric proton pump inhibitor, omeprazole; produced by CYP3A4 sulfoxidation of esomeprazole.

A salen-manganese complex with catalase and SOD mimetic activity.

An inhibitor of HIF-1α protein translation; suppresses phosphorylation of two key regulators of protein synthesis, eukaryotic translation initiation factor 4E binding protein 1 (4EBP1) and p70 S6 kinase; cytotoxic to a variety of cancer cell lines with an IC₅₀ value of 15-25 µM.

An inhibitor of CETP; inhibits plasma CETP with an IC₅₀ value of 9 µM; in rabbits given an atherogenic diet, increases HDL, decreases VLDL, and attenuates induced atherosclerosis; in humans, inhibits CETP activity and increases HDL levels but does not reduce the risk of recurrent…

An agonist of GPR81 (EC₅₀ = 16 µM) that is inactive against the related GPR109a (HCAR2) receptor; stimulates lipolysis (increased serum free fatty acids) in mice fed high fat chow for 10 weeks; blocks basal ghrelin secretion by primary gastric mucosal cells.

A selective agonist of S1P3 (EC₅₀ = 72-132 nM); less effectively activates S1P1 (EC₅₀ = 28-38 µM) and is ineffective at S1P2, S1P4, and S1P5 as well as a panel of other receptors, ion channels and transporters.

An imidazobenzodiazepine derivative that competitively inhibits benzodiazepine binding to GABAA receptors (IC₅₀ = 2 nM); used to reverse sedation induced by benzodiazepine drugs and is effective in the treatment of benzodiazepine overdose or withdrawal.

A HSL compound produced in the marine bioluminescence bacterium V. fischeri.

A natural triterpenoid carboxylic acid that is known to have antioxidative, antimicrobial, anti-inflammatory, and anticancer activities; inhibits Na+/K+-ATPase activity (IC50 = 24.7 μM) and blocks NF-κB activation in various human cancer cells lines (10-100 μM), inhibiting cell…

An immune response modifier that acts as a ligand of TLR7 and 8; demonstrates potent anti-tumor and anti-viral properties and has been used to study the innate immune response to viral infections.

An amino acid derivative and an intermediate, by-product, or modulator of several metabolic pathways, including the activated methyl cycle and cysteine biosynthesis; also a product of SAM-dependent methylation of biological molecules, including DNA, RNA, and histones, and other proteins.

Inhibits smooth MLCK (Ki = 0.3 µM) 10-fold more potently than its parent compound ML-9.

An N-acylethanolamide that inhibits dietary-restriction-induced lifespan extension in wild type and TOR pathway mutant nematodes; also has anti-inflammatory properties, suppressing the expression of IL-6 and MCP-1 in 3T3-L1 adipocytes in response to lipopolysaccharide.

A potent antagonist of the type III receptor tyrosine kinases PDGFRβ, FLT3, and c-Kit (IC₅₀ = 200, 220, and 170 nM, respectively); less potently inhibits CSF-1R (IC₅₀ = 3.4 µM) and does not significantly inhibit other tyrosine or serine/threonine kinases.

The racemic version of the selective NMDA receptor antagonist, D-AP5 that competitively inhibits the glutamate binding site of NMDA receptors (Kd = 1.4 μM); D-AP5 is the active (−)-stereoisomer, while L-AP5, the(+)-isomer, demonstrates considerably less potent NMDA receptor antagonist activity.