An irreversible, noncompetitive inhibitor of PARP1 that disrupts binding between PARP1 and DNA by interacting with the DNA binding domain; produces rapid apoptosis in the various cancer cell (IC50s = 40-128 μM).

A thiazide-like diuretic that targets the Na+-Cl- cotransporter responsible for salt reabsorption in the distal convoluted tubule of the kidney (IC₅₀ = 0.3 µM in rat); inhibits human carbonic anhydrase isoforms VII, XII, and XIII (Kis = 2.1, 5.4, and 15 nM, respectively).

A broad spectrum tyrosine kinase inhibitor that blocks angiogenesis through its actions on VEGFR isoforms; has low nanomolar efficacy against VEGFR1 (FLT1), VEGFR2, VEGFR3 (FLT4), and KIT, as well as CSF1R, PDGFRA, and PDGFRB; effective in vivo and useful in the management of certain types of cancer.

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.

A “hybrid” analog which incorporates components of both the AEA-like and dopaminergic neurotransmitter pathways; is nearly inactive as a TRPV1 ligand and fails to elicit hyperalgesic or nocifensive responses in vivo; exhibits an “entourage” effect at concentrations of 0.1-10…

A potent disruptor of microtubules used as a chemotherapeutic compound; inhibits growth of cervical (HeLa), lung (A549), breast (MCF-7), colon (HT-29), ovarian (OVG-1), and pancreatic (PC-Sh) carcinomas with IC50 values ranging from 2.5-7.5 nM; induces mitotic arrest and initiates apoptosis of…

A potent, stable, and selective agonist analog of AEA with a Ki value of 2.2 nM at the isolated rat CB1 receptor; 325 times more potent at the CB1 receptor compared with the CB2 receptor; induces hypothermia in mice with the same efficacy as AEA, in spite of its much higher affinity for the CB1…

Mn(III)TMPyP is a cell-permeable SOD mimic and peroxynitrite decomposition catalyst. The rate constants for superoxide dismutation and peroxynitrite decomposition are 3.9 x 107 M−1s−1 and ~2 x 106 M−1s−1, respectively.

A substrate for the synthesis of RNA during the transcription process and the synthesis of DNA during DNA replication; participates in G-protein-related signal transduction where it is converted to GDP through the action of GTPases.

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.

An ATP-competitive Pim-1 kinase inhibitor (IC₅₀ = 50 nM) that displays selectivity over the related kinases, Pim-2 and MEK1/2 (IC₅₀s = >20 µM).

A crosslinking reagent that contains NHS ester- and maleimide-reactive groups at the opposite ends of a 4.4 Å spacer arm; used for sequential, two-stage conjugation with amine and sulfhydryl functional groups in the preparation of protein-hapten or protein-protein conjugates.

An elongation product of γ-linolenic acid (18:3), rapidly metabolized by fatty acid desaturases to produce arachidonic acid (20:4); metabolized through the cyclooxygenase pathway to produce 1-series prostaglandins; can reduce atopic dermatitis and atherosclerosis when added to the diet of mice.

A selective SGLT2 inhibitor (IC₅₀ = 3.1 nM) that has been shown in clinical trials of patients with type 2 diabetes to lower fasting and postprandial glucose levels by increasing total glucose excretion, improving β-cell function, and shifting substrate utilization from glucose to lipids.

An anti-inflammatory steroid.

A small molecule radiosensitizer that has proven to be an effective and nontoxic immunochemical hypoxia marker for human squamous cell carcinomas of the cervix, head and neck.

The CysLTs, LTC4 and LTD4, are potent mediators of asthma and hypersensitivity. They induce bronchoconstriction, increase microvascular permeability, and are vasoconstrictors of coronary arteries. Their biological effects are transduced by a pair of GPCRs, CysLT1 and CysLT2. Montelukast (sodium…

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 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.

An antipsychotic compound that displays high affinity for dopamine receptors (Kis = 2.4, 0.2, and 1.8 nM for D2, D3, and D4, respectively); also has actions as an antagonist, inverse agonist, or channel blocker, with lower affinities, at other receptors and channels.

An organic polysulfide compound found in garlic that acts as an H2S donor; reduces the survival of prostate cancer PC-3 cells (IC50 = 22 μM) and inhibits the growth of human colon adenocarcinoma HCT15 cells (IC50 = 11.5 μM); suppresses the growth of PC-3 xenografts in vivo in mice and induces…

An extract from A. lappa, a burdock plant traditionally used in Japanese Kampo medicine for its antioxidant, anti-inflammatory, antiproliferative, and antiviral activity.

A steroid hormone produced in the cortex of the adrenal glands that binds to both glucocorticoid and mineralocorticoid receptors; also is the precursor to aldosterone synthesis.

Functions as a potent laxative by inducing chloride secretion in colonic mucosa and releasing acetylcholine, which stimulates contraction of intestinal smooth muscle; also demonstrates anti-tumor activity (ED50s = 1-13 µM), inducing apoptosis in various cancer cells.

A second generation antiepileptic compound used to prevent convulsions in a variety of settings; binds the synaptic vesicle protein SV2A (pIC₅₀ = 5.7), presumably altering vesicle exocytosis; alters the metabolism and turnover of GABA.

An α-glucosidase inhibitor (IC₅₀ = 5.6 µM) that delays the absorption and digestion of dietary polysaccharides by reversibly inhibiting digestive enzymes such as maltase, isomaltase, and sucrase (IC₅₀s = 0.18, 5.2, and 0.37 µM, respectively).

DETA NONOate is a NO donor. It spontaneously dissociates in a pH-dependent, first-order process with a half-life of 20 hours and 56 hours at 37°C and 22-25°C, pH 7.4, respectively, to liberate 2 moles of NO per mole of parent compound.

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

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.

2-Hydroxymyristic acid is an inhibitor of protein myristoylation requiring about 0.5 mM concentration for full inhibition of acylation.

A succinimide that is converted to N-desmethylmethosuximide, a channel blocker that targets low threshold calcium currents; inhibits CYP2C19-mediated metabolism of biguanides; has anticonvulsant properties in clinical trials.

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.