A small diffusible signaling molecule produced by wild-type E. carotovora strain SCC 3193 involved in quorum sensing, controlling gene expression, and affecting cellular metabolism.

A potent inhibitor of calcium release-activated calcium channels in lymphocytes (IC₅₀ = 100 nM); also inhibits lung IL-4 and CysLT generation in animal models of asthma.

A selective, cell-permeable, reversible inhibitor of MKLP-2 (IC50s = 0.83-1.35 μM); treatment with 10-50 μM results in binucleated cells, perturbing relocation of Aurora B kinase and survivin to the central spindle in anaphase cells without affecting microtubule polymerization.

A selective inhibitor of Δ6 desaturase (IC50 = 0.2 µM in a rat liver microsomal assay) that completely blocks the conversion of linoleic acid to AA; orally active in vivo, decreasing edema in the carrageenan paw edema model in mice.

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,…

A bioactive sterol that can affect cholesterol homeostasis, membrane properties and cell survival; inhibits CYP7A1 with an IC₅₀ = ~ 1 µM; can be used as a standard in the determination of cholesterol derivatives by GC-MS or HPLC.

A potent inhibitor of neprilysin, a membrane metallo-endopeptidase that cleaves peptide hormones, such as enkephalins, glucagon, and bradykinin (Ki = 4-140 nM); produced in vivo via the metabolism of the prodrug acetorphan.

A Bcr-Abl kinase inhibitor (IC₅₀ = 5.8 nM) that is 25- to 55-fold more potent than imatinib in vitro and ≥10-fold more potent in vivo; inhibits 12 out of the 13 most frequent imatinib-resistant Bcr-Abl point mutations, but not the T315I mutation; also targets the Src family kinase Lyn…

A selective PI3K inhibitor with an IC₅₀ value of 1.4 µM.

A quinone derivative that inhibits red blood cell PLA2 with a Ki value of 130 µM.

A potent inhibitor of GSK-3β (IC₅₀ = 22 nM), preventing tau phosphorylation both in vitro and in vivo.

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.…

Linolein hydroperoxides are a mixture of 132 possible isomers of mono-, di-, and tri-hydroperoxides produced from the autoxidation of trilinolein. Autoxidation of linoleic acid containing triglycerides (for example, trilinolein) in vivo could result in the formation of these hydroperoxides. Unlike…

A small molecule inhibitor of tankyrase 1 and 2 (IC₅₀ = 11 and 4 nM, respectively); increases the protein levels of the axin-GSK3β complex and promotes the degradation of β-catenin; inhibits colony formation of APC-deficient colorectal cancer cells at 0.33 µM.

Selectively inhibits MEK1/2; potently inhibits growth and survival of human INA-6 multiple myeloma cells and cytokine-induced osteoclast differentiation (IC50s = 10 and 18.2 nM, respectively); 30 mg/kg reduced tumor growth significantly in mice bearing H929 MM xenografts.

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.

K252c is a cell-permeable PKC inhibitor (IC₅₀s = 2.45 and 25.7 µM for PKC and PKA, respectively). It induces apoptosis in human chronic myelogenous leukemia cancer cells. In human foreskin fibroblast cells, it reduces focus formation induced by human cytomegalovirus (HCMV) strains…

A major oxysterol formed from cholesterol by CYP3A4/5; used as a marker for CYP3A4/5 activity.

An ATP-competitive inhibitor of p38 MAPK isoform p38α (IC₅₀s = 5 nM) and p38β (97% inhibition at 1 µM); has little effect on a range of other kinases, including p38γ and p38δ; blocks the phosphorylation of HSP27, a p38 MAPK substrate, in response to…

An inhibitor of class III receptor tyrosine kinases (IC₅₀s = 0.3 µM for c-Fms, c-Kit, ITD-FLT3 and 1 µM for PDGFRβ); blocks the proliferation of leukemia cells stimulated with FLT3 ligand by preventing the activation of STAT5.

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 purine derivative that reversibly antagonizes aryl hydrocarbon receptor signaling (IC₅₀ = 127 nM in CD34+ cells); induces a 50-fold increase in human embryonic stem cells expressing CD34 (EC₅₀ = 120 nM) and a 17-fold increase in stem cells that retain the ability to engraft…

A naturally-occurring amino acid which is a stable antioxidant; scavenges free radicals and oxidants, controls NF-κB activation, and inhibits inflammatory gene expression; blocks oxidative DNA damage and cell death.

A highly selective inhibitor of PLD1 (IC50 = 3.7 nM) versus PLD2 (IC50 = 6.4 μM).

An active metabolite of propranolol, inhibiting β1- and β2-adrenergic receptors with KD values of 2.4 and 5.8 nM, respectively; comparable to propranolol in potency in antagonizing the effects of isoprenaline on heart rate and blood pressure in cats and dogs.

A selective SIP1 agonist (EC₅₀ = 1.35 nM); activates S1P1-mediated p42/p44 MAPK phosphorylation in CHO-K1 cells transfected with S1P1 (EC₅₀ = 46 nM); induces S1P1-dependent lymphopenia in mice, decreasing B and T cells by 65 and 85%, respectively, at 50 nM.

A benzimidazole analog that inhibits IKK-ε with an IC50 value of ~15.8 µM.

A potent inhibitor of several NHE isoforms, inhibiting NHE1, NHE2, NHE3, and NHE5 with Ki values of 0.02, 0.5, 2.4, and 0.42 μM, respectively; less effectively inhibits NHE4 (IC₅₀ ≥10 μM).

A small molecule inhibitor of DNA ligase IV that prevents nonhomologous end-joining by interfering with the ligase binding and activating apoptosis; inhibits cancer cell growth in vitro (IC₅₀s = 8-120 µM) and in mouse models when co-administered with double-strand break-inducing…

A non-selective bromodomain inhibitor that at 1 µM has been shown to accelerate FRAP recovery of BRD4 and CREBBP bromodomains in HeLa cells.

A quinone which inhibits topoisomerase I at 25 μM and transglutaminase (IC₅₀ = 5 μM); reduced to β-lapachone hydroquinone by NQO1, generating ROS during its reversion to β-lapachone; sensitizes cancer cells to radiation, suppresses NF-κB activation, and drives apoptosis.

An alkaloid metabolite of nicotine as well as a major product of its pyrolysis; binds comparably to CYP2A6 and CYP2A13 (Kis = 7.5 and 5.6 µM, respectively), but appears to more effectively inactivate CYP2A6.