A specific, cell-permeable inhibitor of S6K1 (IC₅₀ = 160 nM); does not inhibit S6K2, MSK, or RSK, or many other unrelated kinases, under conditions in which it inhibits S6K1 activity.

A dietary flavonoid which has diverse physiological activities through both direct and indirect effects; directly binds ERα and ERβ, acting as an inverse agonist or agonist; acts as an antioxidant; suppresses signaling through certain receptor tyrosine kinases, including EGFR and HGF.

A melatonin metabolite first identified in rat brain that has antioxidant and free radical scavenging activities in several experimental models; may be measured in plasma as an index of melatonin synthesis and metabolism.

A prodrug for mycophenolic acid, an inhibitor of inosine monophosphate dehydrogenase; blocks de novo GTP generation as well as RNA and DNA synthesis; inhibits lymphocyte proliferation and activation; used to benefit organ transplantation as well as autoimmunological diseases like lupus.

An inhibitor of p53-Mdm2 interaction (IC50 = 0.09 µM); induces the expression of p53-regulated genes and exhibits potent antiproliferative activity in cells with functional p53.

A potent anti-mitotic drug that is 100-fold more active than resveratrol at inhibiting the growth of human colon cancer Caco-2 cells; inhibits tubulin polymerization in a dose-dependent manner (IC₅₀ = 4 μM) and enzymes involved in the synthesis of the polyamines, putrescine, and spermidine.

A cell permeable derivative of GSH that undergoes hydrolysis by intracellular esterases to release GSH; used to protect cells against damage from radiation, oxidants, and various toxic compounds including heavy metals.

A selective, ATP-competitive inhibitor of the serine/threonine kinase, glycogen synthase kinase 3β (Ki = 38 nM; IC₅₀ = 104 nM); demonstrates neuroprotective effects by inhibiting tau phosphorylation (IC₅₀ = 2.7 μM) at a GSK3-specific site (Ser396) in cells stably…

An anthracycline antitumor antibiotic agent that inhibits DNA topoisomerase II by inducing double-stranded DNA breaks; inhibits nucleic acid synthesis and induces apoptosis by intercalating within DNA.

An activator of the ATP-sensitive K+ channels that displays anti-ischemic (EC25 = 8.9 μM) and cardioprotective (IC₅₀ = 0.03 μM) effects in rat hearts.

NAM is a potent, irreversible inhibitor of MAGL or MAGL-like activity in rat cerebellar membranes, exhibiting an IC50 value of 140 nM. Inhibition of MAGL by the sulfhydryl-reactive maleimide group of NAM suggests a critical cysteine residue is present in the substrate-binding site of the enzyme.

A brain-penetrant inhibitor of CSF1R, as well as c-Kit and FLT3 (IC₅₀s = 20, 10, and 160 nM in vitro, respectively); blocks macrophage recruitment in mammary tumor-bearing mice and blocks glioblastoma invasion in both cell culture and a mouse model of glioblastoma multiforme.

A natural anthocyanidin.

A natural product with anti-inflammatory and cytotoxic activity; inhibits production of TNFα, IL-1β, IL-6, NO, INFγ, and expression of iNOS, and IL-12; blocks human aortic smooth muscle cell migration, inhibits MMP-9 activity, and interferes with PI3K/Akt and ERK1/2 signaling pathways.

DGLA is a metabolite produced by chain elongation of the essential fatty acid γ-linolenic acid. Ethyl DGLA is an esterified version of the free acid which is less water soluble, but more ammenable for the formulation of DGLA-containing diets and dietary supplements. DGLA has been advanced as…

A nonpeptide angiotensin II receptor antagonist which selectively and insurmountably inhibits the angiotensin II AT1 receptor subtype (IC₅₀ = 2.7 nM); does not alter PPARγ activity.

A substrate for cPLA₂.

A potent and selective agonist for both LXRα and LXRβ (EC₅₀ = 50 nM).

Docosatrienoic acid is a rare ω-3 fatty acid not readily detected in normal phospholipid PUFA pools. It inhibits [3H]-LTB4 binding to pig neutrophils at a concentration of 5 µM.

An aminopyridazine derivative that acts as a GABAA receptor antagonist that can be used as an intermediate in the synthesis of SR 95531.

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…

A glucosamine-nitrosourea which is commonly used to induce experimental diabetes in animals; specifically targets beta cells, entering via the glucose transporter GLUT2 and causing alkylation of DNA, leading to the destruction of beta cells.

A non-nucleoside reverse transcriptase inhibitor that binds to viral reverse transcriptase and blocks polymerase activity by preventing RNA plus-strand initiation (IC₅₀s = ~ 0.45 to 0.9 μM).

Blocks mitochondrial complex III; inhibits the activity of the NADH oxidase in certain bacteria.

A benzothiazinone compound that selectively inhibits both MAO-B activity (IC₅₀ = 34.9 nM in human) and adenosine A2A receptors (Ki = 39.5 nM in human); designed as a potential dopamine-sparing therapeutic in the treatment of Parkinson’s disease.

A potent inhibitor of the CK1 isoforms CK1ε and CK1δ (IC₅₀ = 7.7 and 14 nM, respectively); less effectively inhibits a wide variety of related or common kinases; disrupts circadian rhythms in cells and animals; blocks the locomotor response to amphetamines in mice.

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.

A potent and selective AhR antagonist (Ki = 1.2 nM).

A plant lectin that selectively cross-links cell-surface glycoproteins and affects the initiation of cell agglutination, mitogenesis, and apoptosis; widely used in affinity chromatography purifications of various glycoproteins and cellular structures; also used to induce liver injury in…

A derivative of fluphenazine that contains an alkylating chlorethylamine chain, which produces irreversible protein binding; a relatively selective, irreversible antagonist of D2 receptors both in vitro (IC₅₀ = 100 nM) and in vivo; irreversibly inhibits calmodulin at higher doses…

A carboxylic acid-based inhibitor of aldose reductase (IC₅₀ = 0.01-15 μM) that suppresses high glucose-induced proliferation of vascular smooth muscle cells as well as prevents high glucose-induced intracellular NADH/NAD+ increase and membrane-bound protein kinase C activation.

An ATP-competitive Chk1 inhibitor (Ki = 0.49 nM) that demonstrates 100-fold selectivity over Chk2; abrogates DNA damage-induced cell cycle arrest in tumor cell lines and xenografts, potentiating the antiproliferative effects of various chemotherapeutics.