A potent inhibitor of both MEK 1 and 2 that works in an ATP-noncompetitive fashion (IC₅₀s = 0.7 and 0.9 nM, respectively); blocks dual phosphorylation of ERK1/2 and stops cell cycling in cancer cell lines, both in vitro and in multiple tumor models in mice.

2-O-ethyl PAF C-16 is a synthetic PAF analog which contains an ethyl group, attached by an ether linkage, at the sn-2 position. It is a less potent agonist than methylcarbamyl PAF C-16 in the induction of platelet aggregation in both human and rabbit PRP. 2-O-ethyl PAF C-16 causes aggregation of…

A specific inhibitor of class I α-1,2-mannosidase (IC₅₀ = 20 mM), a key enzyme for N-glycan processing in the endoplasmic reticulum and Golgi; inhibiting α-1,2-mannosidase with 1-Deoxymannojirimycin generates N-linked oligosaccharides with high mannose content, preventing…

Hydroxy linoleins are a mixture of 132 possible isomers of mono-, di-, and tri-hydroxy compounds produced by the autoxidation of trilinolein and subsequent reduction of the hydroperoxides. Autoxidation of linoleic acid containing triglycerides (i.e., trilinolein) in vivo could result in the…

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.

Beraprost is an analog of prostacyclin in which the unstable enol-ether has been replaced by a benzofuran ether function. This modification increases the plasma half-life from 30 seconds to several hours, and permits the compound to be taken orally. Doses of 20-100 µg in humans, given 1 to 3…

A stable inhibitor of FAS that leads to profound weight loss and feeding inhibition in both high-fat diet wild type obese and leptin-deficient ob/ob mice.

Piriprost is a structural analog of PGI2 with low IP receptor-mediated activity. Piriprost inhibits 5-LO with an IC₅₀ value around 100 µM, as measured by the release of 5-HETE from cultured myometrial cells. Piriprost inhibits the release of histamine and leukotrienes from isolated…

A selective, ATP-competitive inhibitor of Cdk9, 2, and 7 with IC₅₀ values of 4, 38, and 62 nM, respectively; blocks the cell cycle, inhibits transcription, and induces apoptosis in multiple myeloma RPMI-8226 cells with an IC₉₀ value of 0.3 µM.

Bicyclo PGE2 is a stable, base-catalyzed transformation product of 13,14-dihydro-15-keto PGE2. 13,14-dihydro-15-keto PGE2 itself is a metabolite of PGE2 found in human plasma at a median level of 20-25 pg/ml. Due to the inherent instability of 13,14-dihydro-15-keto PGE2, it is advisable to quantify…

A selective IDO1 inhibitor (IC₅₀ = 7.1 nM in HeLa cells); promotes T and natural killer-cell growth, increases IFN-γ production, and reduces conversion to Treg-like cells in a coculture system of human allogeneic lymphocytes with either dendritic cells or tumor cells; inhibits…

A natural, potent and irreversible inhibitor of cysteine proteases; IC50 values for inhibiting cathepsins K, S, and L, in vitro, are 1.4, 4.1, and 2.5 nM, respectively; also inhibits papain, calpain, and cathepsins B and H.

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).

An FGFR inhibitor.

Linolein hydroperoxides are a mixture of 132 possible isomers of mono-, di-, and tri-hydroperoxides produced from the autoxidation of trilinolein. Autoxidation of linoleic acid containing triglycerides (for example, trilinolein) in vivo could result in the formation of these hydroperoxides. Unlike…

A potent, selective, brain permeable inhibitor of GSK3α and GSK3β (Kis = 6.9 and 31 nM, respectively); shows good bioavailability after oral administration in vivo, inhibiting hippocampal tau phosphorylation and reversing cognitive deficits induced by the NMDA receptor antagonist MK-801.

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

A secondary metabolite produced by fungi; inhibits IgE production by mouse B cells in culture (IC₅₀ = 3.6 μM) and dose-dependently (0.4-25 μg/ml) stimulates neuritogenic activity in rat pheochromocytoma PC12 cells; demonstrates nematicidal activity at 300 μg/ml.

5(Z),11(Z),14(Z)-Eicosatrienoic acid is a PUFA found in various natural sources including maritime pine (Pinus pinaster) seed oil (MPSO), gymnospermae leaves and seeds, and freshwater gastropods. A diet containing MPSO lowered HDL and ApoA1 levels in transgenic mice expressing human ApoA1. MPSO was…

A small molecule pan activator of Ras-related GTPases, activating Rac1, cdc42, Ras, and Rab-2A with EC₅₀ values of 20, 100, 141, and 355 nM, respectively.

O-ASHA is an irreversible, non-selective inhibitor of COX-1 and COX-2. Aspirin is the best-studied example of an irreversible COX inhibitor, acting via the acetylation of the active site serine residue 529 in human COX-1. O-ASHA inhibits ovine COX-1 in a time-dependent, irreversible manner with a…

A colchicine derivative that inhibits tubulin polymerization (IC₅₀ = 2.1 μM) with low toxicity; suppresses microtubule dynamicity, inhibits cell migration, blocks microtubule assembly, and arrests cells in metaphase; used to synchronize cells and for karyotyping in cytogenetic studies.

A broad-spectrum antibiotic that inhibits protein synthesis by inducing miscoding; commonly used as a dominant selection antibiotic for genetically modified bacteria, yeasts, fungi, protozoa, plants, and mammalian cells.

A cell-permeable inhibitor of SCF-mediated c-kit activation, completely blocking phosphorylation of c-kit in human melanoma cells at a concentration between 1 and 5 µM; prevents SCF-mediated downstream phosphorylation of p44/p42 ERK.

A selective inhibitor of the β5i (LMP7) subunit of the immunoproteasome (IC₅₀s = 65 and 73 nM for mouse and human, respectively) that demonstrates significantly weaker activity at the β5 subunit of the constitutive proteasome (IC₅₀s = 0.92 and 1.04 µM for mouse…

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

A selective inhibitor of PDE4 (IC₅₀ = 72 nM) that antagonizes the Hedgehog signaling pathway; activates localized PKA signaling, which, in turn, regulates Gli processing and translocation.

A potent ER antagonist that works by both down-regulating and degrading ERα; efficacious in the treatment of estrogen-sensitive breast cancer; fully activates ER on hippocampal neurons.

A sulfonyl hydrazide that inhibits BCATc (IC₅₀s = 0.81 and 0.2 µM in human and rat, respectively) with 15-fold selectivity over BCATm; blocks calcium influx into neurons (IC₅₀ = 4.8 µM) following inhibition of glutamate uptake and demonstrates neuroprotective…

A synthetic analog of natural PtdIns featuring C8:0 fatty acids at the sn-1 and sn-2 positions; contains the same inositol and DAG stereochemistry as the natural compound.

A selective GPR55 inverse agonist that antagonizes GPR55 constitutive activity (IC₅₀ = 15 μM); blocks GPR55-mediated endothelial wound healing and reverses LPI-inhibited platelet aggregation.

A purine derivative that reversibly antagonizes aryl hydrocarbon receptor signaling (IC₅₀ = 127 nM in CD34+ cells); induces a 50-fold increase in human embryonic stem cells expressing CD34 (EC₅₀ = 120 nM) and a 17-fold increase in stem cells that retain the ability to engraft…