A potent inhibitor that blocks dopamine uptake (IC₅₀ = 1-51 nM); effectively inhibits dopamine uptake in vivo, leading to consequent stimulation of dopamine receptors.

An N-cyanosulphonamide that selectively blocks the sodium/bicarbonate cotransporter (NBC, also known as SLC4A7) with a Ki value of 1.7 µM, with full inhibition occurring at ~30 µM in myocytes; prevents changes in pH associated with depolarization and hyperpolarization of ventricular myocytes.

Formal Name: N-?[[(4-?aminophenyl)?amino]?thioxomethyl]?-?4-?(1,?1-?dimethylethyl)?-benzamide CAS Number: 1011301-27-1 Molecular Formula: C₁₈H₂₁N₃OS

A substrate for cPLA₂.

A natural alkaloid that acts as a selective and reversible α2-adrenergic receptor antagonist (Ki = 12 nM); also acts as a receptor antagonist at the serotonin 5-HT2B receptor (Ki = 14.3 nM).

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is a reversible 5-LO inhibitor that was approved in 1997 for the prevention and treatment of asthma in the USA, but was withdrawn by Abbott Laboratories in 2003.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 natural and potent inhibitor of NEP and NEP2, with Ki values of 2 nM for both enzymes; also a weak inhibitor of the related zinc metalloprotease ECE (Ki = 3.5 µM); has little or no effect on a variety of other proteases.

An inhibitor of Wnt production that impairs Wnt pathway activity (IC₅₀ = 27 nM in vitro) by inactivating Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins; used to suppress embryonic stem cell self-renewal and to decrease cancer cell proliferation,…

A colorimetric substrate whose amino acids YVAD have been shown to be a preferred cleavage site for caspase-1 and -4.

A metabolic precursor of dopamine that crosses the blood brain barrier; used to treat Parkinson’s disease and stroke damage.

A water soluble and metabolically stable curaxin that activates p53 with an EC₅₀ value of 0.37 µM and inhibits NF-κB with an EC₅₀ of 0.47 µM; has broad anticancer activity in mice when administered orally.

A non-nucleoside pyridopyrimidine compound that selectively blocks the action of adenosine kinase in an adenosine-competitive manner (IC₅₀ = 1.7 nM in cell-free assays); suppresses nociception in various rodent pain models.

A macrolide antibiotic with antifungal activity; also cytotoxic against trypanosomes (IC₅₀ = 120-540 ng/ml) while being more than 25,000 times less effective against mammalian cells; inhibits bacterial and mitochondrial ATP synthases.

A natural flavonoid with antioxidant, anti-inflammatory, and anticancer properties; inhibits HIF-1α expression in cancer cells; decreases pro-inflammatory gene expression and oxidative stress in ischemia/reperfusion injury.

A stable, monomethoxylated resveratrol derivative that at 0.1-10 μM reduces neurotoxicity in SH-SY5Y cells induced by the parkinsonian mimetic 6-OHDA and scavenges DPPH radicals (IC₅₀ = 47.1 μM).

Immediate precursor of 4-HNE formed from ω-6 hydroperoxides such as linoleic acid and arachidonic acid.

A 13R,14S-dihydroxy DHA formed by recombinant human macrophage 12-LO and sEH co-incubated with DHA; reduces neutrophil infiltration in a mouse model of peritonitis and enhances human macrophage phagocytosis of zymosan A.

An indoleamine neurohormone whose levels vary in a daily cycle, thereby allowing the entrainment of the circadian rhythms of several biological functions in animals, plants, and microbes; acts as a powerful antioxidant that protects lipids, proteins, and DNA against oxidative damage.

A small molecule inhibitor of nucleophosmin dimers that can prevent cell proliferation and induce apoptosis in various cancer cell lines (IC₅₀s = 1.4-4 µM).

A synthetic thyroid hormone mimetic that lowers total and LDL cholesterol up to 40% when administered to humans at a dose of 50-200 µg once daily for 14 days; stimulates cholesterol catabolism to bile acids without affecting cholesterol synthesis.

A potent and selective dual inhibitor of EGFR and HER2 (IC50s = 19 and 3 nM, respectively); used in combination therapy to prevent or suppress cancers where these kinases are over-expressed, including breast cancer.

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 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).

A stable analog of PFT-α, formed by the condensation of PFT-α in solution; inhibits the growth of the cancer cell lines IGROV-1, A2780, and HCT116 (IC₅₀ = 23, 77, and 103 μM, respectively); induces autophagy in HCT116 cells and sensitizes IGROV-1 and H460 cells to…

A potent inhibitor of HCV infection (EC₅₀ = 17 nM) that displays low cytotoxicity of virally-infected human hepatoma Huh7.5.1 cells (CC₅₀ = 21.3 µM); displays good pharmacokinetics in mice when delivered intraperitoneally, with preferential liver distribution without…

A nonpurine inhibitor of xanthine oxidoreductase (Ki = 0.7 nM) that has proven effective in lowering serum urate levels when administered to manage hyperuricemia in patients with gout.

A dihydropteridinone that inhibits Plk1, Plk2, and Plk3 (IC₅₀s = 0.87, 5, and 56 nM, respectively), inducing mitotic arrest and apoptosis; inhibits proliferation of multiple cancer cell lines (EC₅₀s = 11-37 nM) and prevents the growth of various human carcinoma xenografts in mice.

4-(hydroxymercuri)Benzoic Acid(PHMB) is used to inhibit cysteine-protease and acts as a reversible thiol-specific blocker. While blocking the acylated ghrelin degradation, it allows the AcetylCholine Esterase AChE™ used in SPI-Bio EIA kits to work normally, in contrast to serine-protease inhibitors.

A channel blocker that acts on several TRP channels, including TRPM2, TRPM8, and TRPC6 (IC₅₀ = 1.7, 3.8, and 2.3 μM, respectively); inhibits PLA2, blocking the release of arachidonic acid when given at 50 μM.

An inhibitor of PD-1/PD-L1 interaction.

11β-PGE2 is the C-11 epimer of PGE2. It is a moderate inhibitor of PGE2 binding to rat hypothalamic membranes with a Ki value of 53 nM. 11β-PGE2 also stimulates bone resorption in rats at concentrations of 10-8 to 10-6 M which is similar to PGE2. 11β-PGE2 inhibits PGE2 binding to the…

CAS Number: 940929-33-9 Molecular Formula: C₃₁H₃₃ClN₂O₃ • HCl Formula Weight: 553.5