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

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 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.

ACAT is an intracellular cholesteryl ester synthase tied closely to the absorption of dietary cholesterol. Oleic acid-2,6-diisopropylanilide is an inhibitor of ACAT with an IC50 of 7 nM. When co-administered to rabbits or rats fed a high fat, high cholesterol diet, oleic acid-2,6-diisopropylanilide…

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.

Inhibits smooth MLCK (Ki = 0.3 µM) 10-fold more potently than its parent compound ML-9.

A potent inhibitor of PORCN (IC₅₀ = 74 pM), completely blocking Wnt secretion into culture media; prevents activation of all evaluated Wnt family members; effective in vivo as well as in vitro; blocks the progression of breast cancer while downregulating Wnt/β-catenin pathway target…

A broad spectrum antibiotic that is in the β-lactam subclass known as carbapenems; effective against many Gram-negative and Gram-positive bacteria and is more effective against P. aeruginosa than other carbapenems; not effective against MSRA.

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.

Blocks CYP17A1 by potently inhibiting both the 17α-hydroxylase and the 17,20 lyase activities (IC₅₀ = 18 and 17 nM, respectively); essentially eliminates plasma testosterone while producing a 3- to 4-fold increase in plasma luteinizing hormone.

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.

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 serine proteases inhibitor that is capable of inhibiting trypsin (a digestive system protease; Ki = 15 nM), tryptase (a mast cell protease; Ki = 95.3 pM), and additional proteases in the coagulation cascade including thrombin (Ki = 0.84 μM); 300 mg/kg decreases the total number of eosinophils…

An inhibitor of HIF-1α protein translation; suppresses phosphorylation of two key regulators of protein synthesis, eukaryotic translation initiation factor 4E binding protein 1 (4EBP1) and p70 S6 kinase; cytotoxic to a variety of cancer cell lines with an IC₅₀ value of 15-25 µM.

A quinone derivative that inhibits red blood cell PLA2 with a Ki value of 130 µM.

Ebselen acts as a glutathione peroxidase mimic and is an excellent scavenger of peroxynitrite with a rate constant of 2 x 106 M−1s−1. The glutathione peroxidase-like activity of ebselen inhibits cyclooxygenase and lipoxygenases at micromolar concentrations.

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.

An L-type calcium channel blocker that is selective over N-, R-, P/Q- and T-type calcium channels; displays antihypertensive activity, lowering arterial blood pressure without altering cardiac contractility.

An inhibitor of HMG-CoA reductase (IC50 = 5 nM) that has been shown to be more effective than atorvastatin, simvastatin, or pravastatin in decreasing LDL cholesterol and increasing HDL cholesterol.

An analog of latanoprost in which the hydroxyl at C-15 is inverted relative to latanoprost; binds to the FP receptor in the cat iris sphincter muscle with an IC₅₀ value of 24 µM (tested as the free acid); potential impurity in latanoprost bulk drug preparations.

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…

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

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 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 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 aminonucleoside antibiotic that blocks protein synthesis in both prokaryotes and eukaryotes by causing premature termination of nascent polypeptide chains; used in assays for peptide-bond formation and elongation and also often used as selective agent in cell culture systems.

A selective inhibitor of mutant B-RafV600E (IC₅₀ = 0.8 nM), with 4- and 6-fold reduced potency against wild type B-Raf and c-Raf (IC₅₀s = 3.2 and 5 nM, respectively); studied in clinical trials in patients with B-RafV600E metastatic melanoma and other solid tumors.

A partial receptor agonist of mGlu4, effective at 100 µM, with no activity at other mGlu receptor subtypes; induces apoptosis of T cells at 300-500 µM.

A natural triterpene which stimulates wound healing; induces cell cycle arrest and apoptosis in breast cancer cells (IC50 = 5.9 µM for MCF-7 cells); blocks angiogenesis in glioblastomas; down regulates BACE1 while increasing ADAM10 maturation in primary rat cortical neurons; protects against…

An analytical reference standard categorized as a phytocannabinoid; intended for research and forensic applications

A required cofactor for many enzymes including all NOS isoforms.

An imidazole that potently antagonizes the α2-adrenoceptor (Ki = 1.6 nM); shows selectivity over the α1-adrenoceptor (Ki = 13,300 nM) and is a poor antagonist at a wide variety of other receptors and channels.