A potent and selective AhR antagonist (Ki = 1.2 nM).

An imidazoquinoline compound that activates TLR7 (EC₅₀ = 2.1 µM) on immune cells, inducing the production of IFN-α, IL-12, and other mediators; up-regulates the OGF receptor on cancer cells, blocking cell proliferation (IC₅₀ = 2 µM).

Dihydroartemisinin is a sesquiterpene lactone that can be derived from Artemisia. Dihydroartemisinin exhibits anticancer, antiviral, anti-inflammatory, anti-asthma, and anti-parasitic activities. Artemisinins such as dihydroartemisinin are best known for their antimalarial activity.…

An internal standard for the quantification of oleoyl serotonin by GC- or LC-MS.

A non-ionic detergent commonly used to solubilize membrane-associated proteins; helps retain the native conformation and activity of membrane-associated proteins, and facilitates the reforming of these proteins after denaturation.

A mycotoxin produced from F. moniliforme that functions as an inhibitor of ceramide synthase (sphingosine N-acyltransferase).

Palmitic acid ethyl ester is a neutral, lipid-soluble form of the free acid. It is one of the fatty acid ethyl esters that increase cytosolic Ca2+ concentration leading to pancreatic acinar cell injury due to excessive consumption of ethanol.

A monoacetylated derivative of spermine (Item No. 18041), an endogenous polyamine synthesized from spermidine (Item No. 14918), that displays lower Km and higher Vmax values than spermine, making it a better substrate of polyamine oxidase than the non-acetylated polyamine.

Chlorpheniramine is a first generation alkylamine antihistamine that inhibits H1 histamine receptors, serotonin transporters (SERT), and norepinephrine transporters (NET); it exhibits anti-allergic and antidepressant activities. Chlorpheniramine is clinically used to treat allergic rhinitis and…

Benzo[a]pyrene is a polycyclic aromatic hydrocarbon (PAH) originally found in coal tar, cigarette smoke, and wood smoke. Metabolites of this compound bind DNA and induce mutations. Benzo[a]pyrene is highly carcinogenic and is used in research models to induce carcinogenesis and tumor formation.…

A potent, selective, and competitive inhibitor of ATGL (IC₅₀ = 0.7 μM); does not inhibit hormone-sensitive lipase, monoglyceride lipase, pancreatic lipase, lipoprotein lipase, or other lysophospholipases; blocks lipolysis by ATGL in vitro, in white adipose tissue organ cultures, and…

A LPA analog containing stearyl alcohol at the sn-1 position; exhibits platelet aggregating activity with an EC50 value of 9 nM versus an EC50 value of 177 nM for 1-octadecanoyl LPA.

A major metabolite of PGD2 found in human and mouse urine at levels of approximately 1.5 and 8.1 ng/mg creatinine, respectively.

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.

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…

DuP-697 is a member of the diaryl heterocycle group of selective COX-2 inhibitors which includes MK-966 (rofecoxib), SC-58125, and celecoxib. DuP-697 is a potent and time-dependent inhibitor of COX-2. When tested on isolated recombinant enzymes, DuP-697 is at least 50 times more potent in the…

A selective inhibitor of MEK1 and MEK2 (IC₅₀s = 0.18 and 0.22 μM), the kinases upstream of ERK1/2; rapidly passes the blood-brain barrier and has been used to dissect the effect of RAS/RAF/MEK/ERK signaling pathway inhibition on behavior.

A stable, cell-permeable form of α-ketoglutarate which accumulates rapidly and preferentially in cells with a dysfunctional TCA cycle; stimulates PHD activity and increases HIF-1α turnover when used at 1 mM; competitively blocks succinate- or fumarate-mediated inhibition of PHD.

PGD2 is one of the five primary enzymatic prostaglandins derived directly from PGH2. PGD2 is produced abundantly in the CSF by the lipocalin-type PGD synthase, and in the periphery by myeloid cells including mast cells and basophils by a second, hematopoietic-type PGD synthase. PGD2 is chemically…

A selective inhibitor of TAF1 bromodomain 2 (Kd = 1.8 µM; IC₅₀ = 0.9 µM); synergizes with (+)-JQ1 to inhibit the proliferation of THP-1 and H23 lung adenocarcinoma cells.

CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.

An EpEDE acid formed from DGLA, either by a strong oxidizing agent or by cytochrome P450 epoxygenases; biological properties are poorly understood.

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 specific and potent inhibitor of MPC carrier activity; potently inhibits pyruvate-dependent oxygen consumption by rat heart mitochondria (IC₅₀ = 50 nM).

An Hsp90 inhibitor with an IC₅₀ value of 47 nM; induces the expression of HSP27 and Hsp72 while reducing the client proteins c-Raf, B-Raf, survivin, and PRMT5, causing cell cycle arrest and apoptosis.

13,14-dihydro-15-keto PGF1α is a metabolite of PGF1α that has been reported in the rat stomach. The measurement of 13,14-dihydro-15-keto PGF1α can be used as a marker of the in vivo production of PGF1α.

Bromhexine is a synthetic derivative of vasicine that exhibits mucolytic and antioxidative activities. Bromhexine increases production of serous mucus, decreases mucus viscosity, and helps cilia transport mucus out of the lungs. Bromhexine is clinically used to treat respiratory disorders…

A potent and selective inhibitor of reticulocyte 15-LO-1.

An ethyl ester prodrug of the JMJD3 selective histone demethylase inhibitor GSK-J1; reduces LPS-induced proinflammatory cytokine production, including that of TNFα (IC50 = 9 µM) in human primary macrophages.

A potent agonist of β-adrenergic receptors (pEC₅₀ = 8.13, 8.78, and 6.62 for human β1, β2, and β3, respectively).

An inhibitor of S1P lyase; treatment of mice (50 µg/ml in drinking water) increases lymphoid tissue S1P concentrations 100-fold, reducing lymphocyte egress from thymus and peripheral lymphoid organs, resulting in reversible lymphopenia.

A lipid peroxidation product; actively modifies histidine and lysine residues on proteins and causes protein cross-linking.