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

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

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 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.

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.

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.

Unnatural C-15 epimer of Travoprost.

A metabolite of thyroid hormone.

Activates the aryl hydrocarbon receptor (Ki = 5.4 µM), inducing the expression of both detoxifying enzymes, resulting in pyocyanin degradation, and cytokines that facilitate the clearance of bacteria; accelerates neutrophil apoptosis, resulting in resolution of acute inflammation.

A triazolothiadiazine that inhibits PDE4 (EC₅₀ = 18.7 nM in a cell-based assay); selectively inhibits PDE4A (IC₅₀ = 6.7 nM) over PDE4B1, PDE4B2, PDE4C1, and PDE4D2 (IC₅₀ = 48.2, 37.2, 452, and 49.2 nM, respectively).

A inhibitor of Epac1 and Epac2 (IC₅₀s = 3.2 and 1.4 µM, respectively); blocks Akt phosphorylation and insulin secretion in pancreatic β cells and inhibits the migration of AsPC-1 and PANC-1 pancreatic cancer cells in vitro.

A trypsin-like protease inhibitor known to inhibit trypsin and various inflammatory proteases including plasmin, kallikrein, and thrombin; used in the treatment of chronic pancreatitis and various manifestations of fibrosis.

A bioactive lignan component of P. amarus with antioxidative and hepatoprotective properties; scavenges DPPH radicals (IC50 = 7.4 µM) and alleviates carbon tetrachloride-induced lipid peroxidation and cytotoxicity in a human hepatoma HepG2 cell line.

A cyclododecadepsipeptide potassium-selective ionophore antibotic; induces apoptosis in several cell tyes, including CHO cells, by stimulating potassium efflux.

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 β1-selective adrenoceptor antagonist well known for its cardioprotective and antihypertensive activity; often used to examine the activity of the drug-transporting MDR1 gene product P-glycoprotein.

An aminothiazole that acts as a SIRT-rearranging ligand to selectively inhibit SIRT2 (IC₅₀ = 140 nM) without effect on SIRT1 or SIRT3-6; increases α-tubulin acetylation in HeLa cells.