A water soluble, irreversible, broad spectrum inhibitor of serine proteases, including trypsin, chymotrypsin, plasmin, thrombin, and kallikreins; also inhibits NADPH oxidase.

A natural benzoquinone which directly binds and inhibits XIAP (IC50 = 4.1 μM); blocks growth while activating caspases and promoting apoptosis in cancer cells expressing high levels of XIAP; prevents NF-κB activation by inhibiting IKK; protects against XIAP- and caspase-dependent inflammation.

A NSAID that inhibits COX-1 and -2 activity with IC₅₀ values of 17.4 and 13.1 µM, respectively.

Pargyline is an irreversible inhibitor of monoamine oxidase (MAO) that is used clinically to treat moderate hypertension. At 10 mg/kg iv, pargyline induces a moderate decrease of systolic blood pressure in unanaesthetized hypertensive rats but not normotensive WKR or Sprague-Daley rats. The…

Reversibly binds tubulin and alters GTP hydrolysis as well as microtubule dynamics; nanomolar concentrations reduce both microtubule elongation and shortening velocities, resulting in arrest of cycling in a G2/M phase; also used to induce the formation of Golgi ministacks in eukaryotic cells.

An abundant oligosaccharide in the milk of many mammals, including cows and humans, particularly postpartum; avidly binds several viral strains, including strains of influenza, HIV-1, reovirus, and polyomavirus, in some cases altering viral infectivity.

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 natural intermediate in the pteridine pathway that can be produced naturally from 7-oxobiopterin or in vitro by the oxidation of pterin by xanthine oxidase.

Low potential for eliciting an immune response, ensuring that the primary response is to the antigen-carrier protein conjugate and not against a determinant on the crosslinker. Less immunogenic than SMCC EReactive groups: NHS ester and maleimide Reactive toward: amino and sulfhydryl groups

A natural retinoid that associates with CRBP-I and CRBP-II (Kds = 50 and 90 nM, respectively), which are involved in the intracellular transport of retinol; an intermediate of the phototransduction pathway of photoreceptors; can form toxic conjugates with proteins and lipids, leading to…

Cisplatin is a platinum-based cross-linking agent that exhibits anticancer chemotherapeutic activity. Cisplatin induces crosslinks between guanine bases on DNA; it is clinically used to treat various forms of cancer. In lung cancer cells, cisplatin decreases phosphorylation of PI3K, Akt, and FOXO3a…

An unsaturated fatty acid found in royal jelly produced from honeybees; demonstrates longevity-promoting effects in C. elegans, down regulates matrix metalloproteinases (MMPs) in rheumatoid arthritis, inhibits VEGF-induced angiogenesis in HUVECs, facilitates differentiation of neurons from neural…

A potent and selective PPARγ ligand. It binds to the PPARγ ligand-binding domain with a Kd value of 43 nM.

A competitive antagonist of muscarinic receptors that potently blocks signaling through M1, M2, and M3 (Kis = 25, 125, and 10 nM, respectively), resulting in muscle relaxation.

A membrane-permeable cationic dye that is a substrate for P-gp and is rapidly exported from cells with functional P-gp; also accumulates within mitochondria and can be used to both localize mitochondria and study their properties.

A plant growth regulator involved in the signaling mechanisms for a variety of conditions including plant defense, wound healing, tuberization, fruit ripening, and senescence.

A dual purpose probe; a chemiluminescent probe that detects superoxide production by enzymatic and cellular sources; a fluorescent chloride-sensitive indicator, with fluorescence being quenched by chloride (excitation: 455 nm; emission: 505 nm).

A form of PS that contains the abundant long-chain (16:0) palmitic acid inserted at the sn-1 and sn-2 positions; commonly used in the generation of liposomes and other types of artificial membranes.

A platinum-containing compound that acts as an alkylating agent; used alone or in combination therapy in the treatment of several types of cancer; inhibits the RecA recombinase of M. tuberculosis (IC₅₀ = 2 µM), blocking protein splicing and cell growth.

An NMDA open-channel blocker (Ki = 1.2 μM at -60 mV) and uncompetitive antagonist with known anti-Parkinsonian, anti-epileptic, anti-stroke, and anti-Alzheimer’s disease properties; 12 μM blocks 90% of NMDA receptor activity and prevents NMDA-receptor mediated neurotoxicity in rat…

A GABAA receptor agonist whose potency varies depending on the receptor subunit composition (partial agonist at α1β2γ2 (ED50 = 143 µM), full agonist at α5 (ED50 = 28-129 µM), and super agonist at α4β3δ (ED50 = 6 µM)); acts as an antagonist…

A reversible inhibitor of serine proteases such as trypsin (Ki = 0.06 pM), chymotrypsin (Ki = 9.5 nM), and kallikrein (Ki = 0.8 nM); widely used as a protein purification tool to prevent proteases present in tissue samples from degrading the protein of interest.

A fluorescent indicator of peroxynitrite formation; neither NO, superoxide, nor hydrogen peroxide alone appear to oxidize DCFH.

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

An intermediate in the synthesis of cysteine that is produced from homocysteine and serine by the action of cystathionine-β-synthase; excess cystathionine in the urine is a hallmark of cystathioninuria.

N-Acetyl-S-(N’-phenylthiocarbamoyl)-L-cysteine (PITC) is a cysteine conjugate of N-acetyl-phenylisothiocyanate. Isothiocyanates are typically found in plants of the Brassicaceae family, including broccoli, cabbage, and radish. Isothiocyanates are best known for their antioxidative, anticancer…

The primary active component of the heat and pain-eliciting lipid-soluble fraction of the Capsicum pepper and present in natural hot pepper extracts; elicits a sensation of burning pain by activation of TRPV1 on small, non-myelinated polymodal C-type nociceptive nerve fibers and has been widely…

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 non-nucleoside DNA methyltransferase inhibitor (IC₅₀ = 115 nM in vitro) that significantly reduces the methylation of genomic DNA in cells at 10 μM without detectable toxicity.

A potent inhibitor of ROCK-II, PRK-2, MSK1, and MAPKAP-K1b with IC50 values of 1.9, 4, 5, and 15 µM, respectively; has been shown to reduce blood vessel constriction, decreases pulmonary arterial pressure, inhibit tumor angiogenesis, and improve insulin signaling in a diabetic rat model; drug…

A thiol-reactive fluorogenic probe; used to evaluate or quantify a variety of compounds containing reactive sulfur or thiol groups, including H2S, glutathione, proteins, and nucleotides.

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…