Angiotensin II is a hormone that plays an important role in regulating blood pressure. Elevated levels of angiotensin II are implicated in inducing and maintaining hypertension, and also in the development of atherosclerosis. Both of these effects are mediated by the angiotensin II type 1 (AT1)…

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 variety of natural products from plant sources, particularly flavonoids, have long been observed to have antioxidant activity with potential benefits for human health. Antioxidant triterpenes are less common. Celastrol is a triterpenoid antioxidant compound isolated from the Chinese thunder god…

An antithrombic compound whose active metabolite is a selective, irreversible antagonist of the platelet purinergic P2Y12 receptor (IC₅₀ = 100 nM); inhibits ADP-induced platelet aggregation ex vivo; shown to be beneficial in the prevention of vascular ischemic events for patients without…

A dietary flavonoid which has diverse physiological activities through both direct and indirect effects; directly binds ERα and ERβ, acting as an inverse agonist or agonist; acts as an antioxidant; suppresses signaling through certain receptor tyrosine kinases, including EGFR and HGF.

A nuclesoside analog that disrupts DNA synthesis in blood cells; effective in a number of animal tumor systems including LI210 leukemia, CD8F mammary adenocarcinoma, P388 leukemia, and human LX-1 lung tumor xenograft and displays anticancer activity against human hematological malignancies in vivo.

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-ionic, water-soluble X-ray contrast agent for intravascular administration; can cause acute kidney injury and is used in animal models of contrast-induced nephropathy.

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

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.

A potent and selective CB1 receptor inverse agonist (Ki = 243 nM; EC50 = 195 nM); a 10 µM concentration results in 100% and 35% displacement of [3H]-CP-55,940 at the CB1 and CB2 receptors, respectively.

1-Oleoyl lysophosphatidic acid is a species of LPA containing oleic acid at the sn-1 position. Phosphatidic acid is produced either directly through the action of PLD or through a two step process involving liberation of DAG by PLC followed by phosphorylation of DAG by diglycerol kinase.{2656}…

A highly potent, reversible inhibitor of the EGFR (Ki = 5.2 pM; IC₅₀ = 29 pM); rapidly suppresses autophosphorylation of EGFR in ?broblasts and human epidermoid carcinoma cells.

A selective inhibitor of PFKFB3 (IC₅₀ = 207 nM); rapidly induces apoptosis in transformed cells, suppresses glucose uptake and growth of Lewis lung carcinomas in syngeneic mice, and yields antitumor effects in human xenograft models of cancer in athymic mice.

An intermediary prodrug of fluorouracil, the pyrimidine analog that inhibits thymidylate synthase selectively in tumor cells, interfering with DNA synthesis; one of two intermediary metabolites formed during metabolic conversion of the chemotherapeutic prodrug, capecitabine, to fluorouracil.

Carboxy-PTIO is a NO scavenger. It reacts stoichiometrically with NO and can be used for EPR detection of NO.

A natural product with anti-inflammatory, anti-tumor, and neuroprotective effects; inhibits GSK-3 (IC₅₀ = 2.5 μM) and Cdk1 and 5 (IC₅₀ = 10 μM for both isoforms).

A dual inhibitor of c-Src and Abl (IC50 = 2.7 and 30 nM, respectively); less effectively inhibits other kinases; blocks cell motility, migration, adhesion, invasion, proliferation, differentiation, and survival; reduces osteoclast bone resorption.

An inhibitor of Ras-mediated signaling that inhibits the growth of PANC-1 and U87 tumor cells with IC₅₀ values of 20 and 10 µM, respectively.

A form of the myristic acid that is found in the lipid A component of some Gram negative bacteria, including Escherichia, Haemophilus, Actinobacillus, and Campylobacter species.

An inhibitor of both CDK1 and CDK2 (IC₅₀s =2.9 and 2.2 µM, respectively); inhibits cellular ataxia telangiectasia mutated and Rad3-realted kinase activity (IC₅₀ = 6.7 µM) and impairs G2/M arrest in various human cancer cells, potentiating the cytotoxic effects of…

An apigenin flavone C-glycoside isolated from various tropical plant species that demonstrates broad antioxidant, anti-inflammatory, anticancer, and antinociceptive activities.

A benzothiazole derivative with anti-excitotoxic effects that acts by blocking the presynaptic release of glutamate, indirectly antagonizing glutamate receptors, and inactivating neuronal voltage-gated Na+ channels (ED50 = 2.3 μM); suppresses glutamate-induced seizures in rats (ED₅₀ =…

A cell-permeable, cGMP analog that activates cGMP-dependent protein kinase.

An inhibitor of p53-Mdm2 interaction (IC50 = 0.09 µM); induces the expression of p53-regulated genes and exhibits potent antiproliferative activity in cells with functional p53.

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…

An oxidizing reagent that reacts with nitric oxide to form nitric dioxide and corresponding imino nitroxides.

A corticosteroid prodrug that is converted to its active form, des-CIC, a glucocorticoid receptor agonist (Ki = 0.31 nM); used to ameliorate symptoms of airway inflammatory diseases.

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 selective inhibitor of human collagenase-3, also known as MMP-13, producing 89% inhibition at 10 µg/ml; used to evaluate the role of MMP-13 in diverse processes.

A selective ERRβ/γ receptor agonist (EC₅₀ = 130 nM); used to potentiate ERRγ-induced growth inhibition in LNCaP and DU145 prostate cancer cell lines.