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

Raclopride is a selective dopamine D₂/D₃ receptor antagonist with K_i values of 1.8, 3.5, 2,400, and 18,000 nM for D₂, D₃, D₄, and D₁ receptors, respectively. It passes the blood brain barrier and can be used in in vivo…

A selective, ATP-competitive inhibitor of Cdk9, 2, and 7 with IC₅₀ values of 4, 38, and 62 nM, respectively; blocks the cell cycle, inhibits transcription, and induces apoptosis in multiple myeloma RPMI-8226 cells with an IC₉₀ value of 0.3 µM.

The ethanolamine amide of DHA that has been detected in both brain and retina at concentrations similar to those for AEA; binds to the rat brain CB1 receptor (Ki = 324 nM), which is approximately 10-fold higher than the Ki for AEA; inhibits shaker-related voltage-gated potassium channels in brain…

A fluorescent probe commonly used to identify dead cells; excitation at 488-535 nm and emission maximum of 617 nm.

A metabolite of vitamin A that acts as a ligand for both the RAR and the RXR.

A competitive inhibitor of heme oxygenase that also inhibits soluble guanylyl cyclase and inactivates the NOS isoforms nNOS, iNOS, and eNOS (IC₅₀s = 0.8, 4, and 5 μM, respectively); used to assess iron status and to diagnose iron disorders and has shown therapeutic potential in hyperbilirubinemia.

A derivative of testosterone and ethisterone that binds androgen receptors and sex hormone-binding globulin causing a 3-fold increase in free testosterone; possesses weak androgenic effects and inhibits the production of gonadotropins.

A potent inhibitor of PDE5 (IC50 = 1-5 nM) that also blocks the activity of PDE11 (IC50 = 10-33 nM); IC50 values against other isoforms of PDE are in the micromolar range; pharmacokinetics are highlighted by its prolonged duration of effect.

A conjugate of biotin and lysine used for derivatization or conjugation to proteins and other molecules with a medium-chain length spacer; also used as an anterograde, retrograde, or intracellular neuroanatomical tracer that is fixable with aldehyde-based fixatives.

An imidazotetrazine that is converted to a compound capable of alkylating DNA, thus interfering with DNA replication and leading to cytotoxicity in proliferating cells; rapidly and completely absorbed from the gastrointestinal tract after oral administration and readily crosses the blood-brain barrier.

3-Tert-butyl-4-hydroxyanisole (3-BHA) is one component of butylated hydroxyanisole (BHA). This compound is commonly used as a food additive; it exhibits antioxidative and anticancer activities. In leukemia cells, 3-BHA decreases the mitochondrial membrane potential, inhibits mitochondrial oxidative…

Cilostazol is a quinolone inhibitor of phosphodiesterase 3B (PDE 3B) that exhibits vasodilatory, antiplatelet, anti-inflammatory, anti-diabetic, antidepressant, anxiolytic, and pro-angiogenic activities. Cilostazol is clinically used to treat intermittent claudication associated with peripheral…

A potent TRPV1 antagonist that inhibits capsaicin-induced and acid-induced activation of rat TRPV1 with IC50 values of 35 and 6 nM, respectively.

MAHMA NONOate is a NO donor. It spontaneously dissociates in a pH-dependent, first-order process with a half-life of 1 minute and 3 minutes at 37°C and 22-25°C, respectively, (pH 7.4) to liberate 2 moles of NO per mole of parent compound.

A potent, selective antagonist of the β2-adrenergic receptor (Ki = 0.7 nM for the β2 receptor, compared with 49.5 and 611 nM for β1 and β3 receptors, respectively); active in vivo and often used to evaluate the actions of adrenergic receptor agonists.

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.

A post-synaptic α1-adrenergic receptor antagonist commonly used to improve lower urinary tract symptoms associated with benign prostatic hyperplasia; displays high-affinity with non-selectivity for the three known human α1 adrenoceptors (pKi = 8.0, 8.0, and 8.5 for α1A, α1B,…

A potent and selective inhibitor of reticulocyte 15-LO-1.

A selective antagonist of S1P binding to the S1P3 receptor; blocks calcium increase in HeLa cells by about 40% at 10 µM.

A cell-permeable, stable free radical that is commonly used to evaluate the ability of compounds to act as free radical scavengers or hydrogen donors and to measure the antioxidant activity of tissue extracts; followed by color change from purple (absorbance at 515-528 nm) to yellow.

A second generation analog of amiloride that inhibits TRPP3-mediated Ca2+-activated (IC₅₀ = 0.14 μM) and ENaC (IC₅₀ = 10 nM); inhibits active sodium transport of human and ovine bronchial epithelial cells (IC₅₀s = 75 and 116 nM, respectively).

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.

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 natural polymethoxylated flavonoid and potent antioxidant with good bioavailability; has anti-inflammatory effects that are relevant to a host of diseases, including cancer, arthritis, and neurodegeneration; inhibits P-glycoprotein and BCRP (IC₅₀ = 11.5 and 4.9 μM, respectively).

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.

Oleyloxyethyl phosphorylcholine is an inhibitor of PLA2 with an IC₅₀ value of 6.2 µM for porcine pancreatic PLA2.

A potent inhibitor of tubulin polymerization with strong inhibitory activity on tumor cell growth.

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 monoacetylated derivative of spermine (Item No. 18041), an endogenous polyamine synthesized from spermidine (Item No. 14918), that displays lower Km and higher Vmax values than spermine, making it a better substrate of polyamine oxidase than the non-acetylated polyamine.

Zileuton (Zyflo™) is a reversible 5-LO inhibitor that was approved in 1997 for the prevention and treatment of asthma in the USA, but was withdrawn by Abbott Laboratories in 2003. Zileuton inhibits 5-LO from rat basophilic leukemia-1 (RBL-1) cells with an IC50 value of 0.5 µM. It is a…

A DNA alkylating agents that induces DNA interstrand and intrastrand crosslinks, cytotoxicity, and apoptosis; inhibits the growth of PC-3 prostate cancer cells with IC₅₀ values of 0.074 or 0.77 μM for sequential dosing or single dosing, respectively.