A methylsulfanylimidazole that inhibits p38 MAP kinase (IC₅₀ = 0.90 µM in vitro); potently blocks the release of TNF-α and IL-1β from human peripheral blood mononuclear cells (IC₅₀s = 0.37 and 0.044 µM, respectively).

13,14-dihydro-19(R)-hydroxy PGE1 is the theoretical metabolite of 13,14-dihydro PGE1 by ω-1 hydroxylase. There are no known reports on its biosynthesis or biological activity.

AD140 is an orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM) that binds to the androgen receptor with a Ki value of 7 nM. At 0.03-0.3 mg/kg, it has been shown to stimulate muscle weight increase without affecting prostate or seminal vesicle in castrated male rats. At…

A toxin produced by cyanobacteria that inhibits the catalytic activity of protein phosphatases PP1C, PP1γ, and PP2A with Ki values of 0.15, 0.24, and 0.018 nM, respectively.

A hydrophobic diterpene ester that rapidly induces cell death in proliferating keratinocytes through plasma membrane and mitochondrial disruption; causes inflammation due, at least in part, to activation of PKC, leading to antibody-dependent cellular cytotoxicity.

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 fluorogenic substrate for chitinases and chitotriosidases.

A structurally unusual antibiotic that inhibits NADH-dependent enoyl (Acyl-Carrier-Protein) reductase InhA, preventing mycolic acid synthesis in M. tuberculosis, including isoniazid-resistant strains (MICs = 0.31-0.63 µg/ml).

An internal standard for the quantification of 5-POHSA by GC- or LC-MS.

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…

8-iso PGA1 is an isoprostane and a member in a large family of prostanoids of non-cyclooxygenase origin. It occurs as a common minor impurity in most commercial preparations of PGE1. The biological activity of 8-iso PGA1 has not been studied in depth or reported in the literature.

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.

11β-PGF2α-d4 contains four deuterium atoms at the 3, 3', 4, and 4' positions. It is intended for use as an internal standard for the quantification of 11β-PGF2α by GC- or LC-MS.

A fluorogenic substrate of palmitoyl-protein thioesterase.

A regioisomeric resveratrol metabolite that may be used as a reference standard for accurate determination of the metabolic profile of resveratrol.

A metabolite of estradiol 3-sulfate that has been modified by a UDP-glucuronosyltransferase; enhances utilization by anion transporters, most commonly leading to excretion in urine and bile.

A chromogenic substrate for endoglucanases and cellobiohydrolases.

An internal standard for the quantification of 17β-estradiol by GC- or LC-MS.

A hepatic metabolite of zearalenone that is a less potent agonist of estrogen receptors than the parent compound.

Iloprost is a second generation structural analog of prostacyclin (PGI) with about ten-fold greater potency than the first generation stable analogs, typified by carbaprostacyclin. Iloprost binds with equal affinity to the human recombinant IP and EP1 receptors with a Ki of 11 nM. Iloprost…

A β3-adrenoceptor agonist (EC₅₀ = 3 nM) that is >10,000-fold selective over β1 and β2; causes a rapid decrease in blood glucose level in mice and has been used to study the induction of brown adipocytes and to increase thermogenesis in a mouse model of dietary obesity.

A synthetic version of the endogenous antidiuretic hormone arginine vasopressin; acts as an agonist at human vasopressin V1a, V1b, and V2 receptors with Ki values of 62.4, 5.8, and 23.3 nM, respectively.

Largely acts a cell signaling intermediate; serving as substrate to produce IP5s, which can be further phosphorylated to produce Ins(1,2,3,4,5,6-)P6; also phosphorylated to produce phytic acid, which serves diverse roles in eukaryotic tissues; a poor activator of the Ins(1,4,5)-P3 receptor in vitro.

A potent inhibitor of PKC (IC₅₀ = 2.7 nM for the rat brain enzyme).

Reversibly and selectively blocks Tie2 kinase activity (IC₅₀ = 250 nM); reduces angiogenesis in a Matrigel neovascularization assay and delays tumor growth in MOPC-315 plasmacytoma and SVR angiosarcoma xenograft models.

A pyrazine derivative that is used as a flavoring agent in the food and tobacco industry; has DNA strand breakage activity and strongly inhibits IL-2 production by Jurkat cells stimulated with phytohemagglutinin (IC₅₀ = ~1.25 mM).

A PARP1 inhibitor (IC₅₀ = 450 nM) that displays neuroprotective effects in cultured mouse cortical neurons; also inhibits eosinophilic infiltration into airways of OVA-challenged mice and induces the regression of atherosclerotic plaques in high-fat fed ApoE(-/-) mice.

An analog of ceramide that inhibits alkaline ceramidase (IC50 ~5 µM); suppresses growth of HL-60 cancer cells in culture.

A natural kavalactone that enhances the binding of bicuculline methochloride at the GABAA receptor at 0.1 µM.

A DHA epoxygenase metabolite detected in rat brain and spinal cord, as well as human serum, that acts as a substrate for sEH (Km = 5.1 µM); demonstrates antihyperalgesic activity in inflammatory and neuropathic pain models and potently inhibits angiogenesis and tumor growth in in vitro assays.

The physiological actions of PGD2 include regulation of sleep, lowering of body temperature, inhibition of platelet aggregation and relaxation of vascular smooth muscle. PGD2 mediates its effects by 2 distinct G-protein-coupled receptors, DP1 and CRTH2/DP2. 15(R)-15-methyl PGD2 is a potent,…