PGF2α 1,15-lactone is a lipid-soluble internal ester of PGF2α. Hydrolysis of the lactone readily produces free PGF2α in plasma. In rhesus monkeys, a total dose of 15 mg of PGF2α 1,15-lactone terminates early pregnancy, whereas PGF2α is ineffective.

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 cell permeable, peptide aldehyde inhibitor of calpain I (Ki = 120 nM), calpain II (Ki = 230 nM), cathepsin B (Ki = 100 nM), and cathepsin L (Ki = 0.6 nM).

An active, deacetylated metabolite of T-2 toxin; inhibits protein synthesis and cell proliferation in plants; causes acute and chronic toxic effects in animals that ingest contaminated plant materials.

A kaempferol glycoside that selectively inhibits RSK2 with an IC50 value of 89 nM (Ki = 1 μM) without interfering with upstream activators of RSK, including ERK, MEK, EGFR, and PKC; inhibits the proliferation of MCF-7 breast cancer cells at 100 μM and attenuates angiotensin II-induced cell…

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 internal standard for the quantification of (±)-β-hydroxybutyrate (sodium salt) by GC- or LC-MS.

A potent and selective competitive antagonist of the EP1 receptor (Ki = 0.6 and 1.7 nM for human and mouse EP1, respectively); effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer; suppresses pain and acid-induced HCO₃- secretion in the stomach.

A cell-permeable inhibitor that binds actin filaments, but not actin monomers, to inhibit polymerization at concentrations as low as 0.2 µM.

A competitive inhibitor of CBX7 chromodomain binding to H3K27me3 (Ki = 43 µM); derepresses transcription of the polycomb repressive complex target gene p16/CDKN2A in prostate cancer cells at 250 µM.

A derivative of glucose used to study carbohydrate metabolism, particularly in the identification, differentiation, and characterization of α-phosphoglucomutase, β-phosphoglucomutase, and α- and β-hexoglucomutases.

An antagonist of GPR55, blocking LPI-induced activation (EC₅₀ = 1.1 µM); has minimal effect at the GPR35 and CB2, although it acts as a weak antagonist of CB1 (IC₅₀ = 17.7 µM); inhibits LPI-induced phosphorylation of ERK1/2 and blocks receptor-dependent…

Endogenous ligand of the APJ receptor, with an EC50 of 0.37 nM; acts primarily in the periphery and CNS, playing important roles in regulating cardiovascular function, fluid homeostasis, hypertension, and insulin sensitivity.

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 potent, selective inhibitor of ATR (IC₅₀ = 5 nM); inhibits the growth of LoVo colorectal adenocarcinoma cells in vitro and significantly reduces the growth of LoVo xenografts in mice.

An enantiomer of atorvastatin that has little or no inhibitory activity against HMG-CoA reductase.

A covalent Cdk7 inhibitor (IC₅₀s = 3.2-15.6 nM in vitro) that displays broad anti-proliferative activity against cancer cell lines, particularly T-ALL cell lines with characteristic misregulation of T cell lineage-specific transcription factors.

A grasshopper neuropeptide from a family of arthropod hormones and neuroregulators, found in Locusta migratoria.

FR122047 is a selective inhibitor of COX-1. The IC50 values for inhibition of human COX-1 and COX-2 are 0.028 and 65 µM, respectively. In human platelet-rich plasma, FR122047 inhibits arachidonic acid, collagen, and ADP-induced platelet aggregation with an IC50 of 180-200 nM, which is nearly…

An activator of the HIF signaling pathway, as demonstrated by HRE reporter assay (EC₅₀ = 1.2 µM), HIF-1α nuclear translocation assay (EC₅₀ = 1.3 µM), and increased VEGF expression (EC₅₀ = 1.6 µM); activity is blocked by excess iron,…

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…

An allosteric, reversible inhibitor of PAR1 on platelets, preventing surface expression of P-selectin induced by the peptide SFLLRN with an IC₅₀ value of 0.26 µM; also blocks platelet activation induced by thrombin but not by PMA, U-46619, or collagen.

A selective slow off-rate inhibitor of Raf kinases (IC₅₀s = 8.3, 2.4, and 1.4 nM for wild type B-Raf, mutant B-RafV600E, and c-Raf, respectively); shows significant antiproliferative activity against mutated BRAF or mutated NRAS cancer cell lines and xenograft models.

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.

An antagonist of Bcl-2 family members containing four Bcl-2 homology domains, including Bcl-2, Bcl-W, Bcl-xL, and Mcl-1 (Kd ~500 nM); prevents interaction of these pro-survival proteins with Bax or Bak, inducing apoptosis; also induces autophagy in mouse embryo fibroblasts and in HeLa cell.

A natural type B trichothecene produced by certain species of the fungus Fusarium; inhibits protein biosynthesis, binds to peptidyl transferase, and inhibits the synthesis of RNA and DNA; passes the blood-brain barrier at different rates in different animals.

An organophosphorus ester that antagonizes the CB1 receptor and inhibits FAAH with similar potencies (IC50s = 2 nM).

A highly selective inhibitor of PLD1 (IC50 = 3.7 nM) versus PLD2 (IC50 = 6.4 μM).

A potent, selective, and cell-permeable inhibitor of the BRPF1 bromodomain (IC₅₀ = 80 nM); disrupts chromatin binding of BRPF1 in a cellular assay by blocking the interaction of BRPF1 with histone H3.3.

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.

9β-hydroxy stereoisomer of PGF2α; much less active than PGF2α in antifertility and bronchoconstrictor activities; exhibits bronchodilating activity in guinea pigs and cats and antagonizes the bronchoconstrictor activity of PGF2α.

An antibiotic that suppresses the expression of ODC, COX-2, and iNOS at concentrations as low as 0.3 μM and exhibits an anti-metastasis effect and anti-tumor promoter activity in various carcinogenesis mouse models.