A selective inhibitor of CaMKII, competitively blocking CaM binding to the kinase (Ki = 370 nM); inhibits histamine-induced aminopyrine uptake in parietal cells (IC₅₀ = 300 nM).

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 cell-permeable inhibitor of sirtuin NAD+-dependent deacetylases, inhibiting the yeast sirtuin Sir2p with an IC50 value of 68 μM and the human sirtuins SIRT1 and SIRT2 with IC50 values of 131 and 38 μM, respectively; does not alter HDAC1 activity.

A stable analog of ATP that acts as a potent agonist of G protein-coupled P2Y2 and P2Y11 receptors (pEC₅₀ = 5.52 for P2Y11).

Initiates glycogen synthesis in hepatocytes by causing inactivation of phosphorylase a and activation of glycogen synthase a (maximal effects with ~20 µM Itu); potent inhibitor of ERK2 (Ki = 525 nM).

PGF1α is the putative metabolite of DGLA via the COX pathway. Both PGF1α and PGF2α have been shown to act as priming pheromones for male Atlantic salmon with a threshold concentration of 10−11 M. PGF1α binds to the ovine corpus luteum FP receptor at only 8% of the…

A naturally-occurring amino acid which is a stable antioxidant; scavenges free radicals and oxidants, controls NF-κB activation, and inhibits inflammatory gene expression; blocks oxidative DNA damage and cell death.

A protein cross-linking agent isolated from G. jasminoides Ellis; inhibits UCP2 activity; 5 µM genipin increases glucose-stimulated insulin secretion in isolated pancreatic islets chronically exposed to high levels of glucose; induces apoptosis in FaO rat hepatoma cells and human…

A full antagonist of estrogen ERβ receptors with 36-fold selectivity over ERα (relative binding affinities are 0.01 and 0.36, respectively); enhances SKOV3 and OV2008 ovarian cancer cell growth in in vitro assays at 100 pM.

A cyclic nitrone spin trap that can be used for the detection and characterization of thiyl radicals, hydroxyl radicals, and superoxide anions in vitro or in vivo.

A potent, selective chemical probe for the methyl lysine reading function of L3MBTL3 (Kd = 120 nM; IC₅₀ = 40 nM) that competitively displaces mono- or dimethyl-lysine containing peptides.

A small molecule radiosensitizer that has proven to be an effective and nontoxic immunochemical hypoxia marker for human squamous cell carcinomas of the cervix, head and neck.

A small molecule inhibitor of DNA ligase IV that prevents nonhomologous end-joining by interfering with the ligase binding and activating apoptosis; inhibits cancer cell growth in vitro (IC₅₀s = 8-120 µM) and in mouse models when co-administered with double-strand break-inducing…

6-keto prostaglandin F_1α (6-keto PGF_1α) is the inactive, non-enzymatic hydrolysis product of PGI₂. 6-keto PGF_1α serves as a useful marker of PGI₂ biosynthesis in vivo. When [ 3 H]-PGI₂ is injected into healthy human…

A flavonoid isolated from the root of the traditional Chinese herb S. baicalensis with anti-inflammatory, antioxidant, antitumor, and neuroprotective activities at concentrations from 5-75 μM.

A TZD that increases the sensitivity of cells to insulin, stimulating insulin-induced PI3K activity at submicromolar concentrations; increases insulin effectiveness in obese NIDDM subjects; promotes adipocyte differentiation by up-regulating the expression of UCP-2.

A selective antagonist of BET bromodomains, binding with 10-100-fold higher affinity for BD2 (IC₅₀ = 0.04-0.28 µM) over BD1 (IC₅₀ = 1.8-3.1 µM), which causes selective release of BET proteins from chromatin; increases the expression of ApoA1 and reduces…

An estrogen metabolite that acts as a substrate of MRP2 (Km = 75 µM), and through MRP2-mediated transport, functions as a cholestatic agent, decreasing bile flow.

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…

A hydrolyzable tannin with phytotoxic activity.

An alkaloid metabolite of nicotine as well as a major product of its pyrolysis; binds comparably to CYP2A6 and CYP2A13 (Kis = 7.5 and 5.6 µM, respectively), but appears to more effectively inactivate CYP2A6.

An indole diterpene which potently and reversibly inhibits large conductance Ca2+-activated K+ (BKCa) channels, as shown in patch clamp (Ki = 1.9 nM) and whole smooth muscle cell studies (Ki = 35.7 nM).

A cell-permeable selective inhibitor of the PI3K catalytic subunit p110δ (IC50 = 0.5 μM). It less effectively inhibits p110γ and p110β (IC50 = 29 and 75 μM, respectively) and has no significant effect on p110α and several other kinases.

A natural alkaloid that inhibits protein synthesis at low micromolar concentrations; immobilizes ribosomes immediately after the initiation of translation.

A bioactive saponin used in traditional Chinese medicine; has diverse protective effects for the cardiovascular, immune, digestive, and nervous systems.

A pyridine regio-isomer of the JMJD3 inhibitor GSK-J4; cell-permeable and hydrolyzed to a free base, which is a weak inhibitor of JMJD3 (IC50 > 100 μM), making it an ideal negative control molecule.

An intermediate in the HMG-CoA reductase pathway derived directly from farnesyl pyrophosphate and used in the biosynthesis of terpenes and terpenoids; also serves as a substrate in the prenylation of a variety of critical intracellular proteins including small GTPases.

An inhibitor of SAH hydrolase; depletes EZH2 levels and inhibits trimethylation of lysine 27 on histone H3 in acute myeloid leukemia cells in a dose-dependent manner (0.2-1 μM); increases expression of the cell-cycle regulators p21, p27, and FBXO32 leading to cell cycle arrest and apoptosis.

16,16-dimethyl PGF2β is a metabolically stable analog of PGF2β. It prevents bronchospasm in asthmatics but is less potent than PGE2.

A substrate for β-galactosidase, the lactose repressor, the galactose-binding protein, the β-methylgalactoside transport system, and thiogalactoside transacetylase.

11β-PGE1 is an epimerized form of PGE1 at the C-11 position. 11β-PGE1 is a less potent isomer of PGE1. It is 13% and 3.6% as potent as PGE1 in contracting the rat uterus and guinea pig ileum, respectively.

A fluorogenic substrate of palmitoyl-protein thioesterase.