The ethanolamine amide of DHA that has been detected in both brain and retina at concentrations similar to those for AEA; binds to the rat brain CB1 receptor (Ki = 324 nM), which is approximately 10-fold higher than the Ki for AEA; inhibits shaker-related voltage-gated potassium channels in brain…

8-iso PGF1β is a potential autoxidation product of DGLA. There are no published reports on its isolation from any biological source or on its biological activity.

An apigenin flavone C-glycoside isolated from various tropical plant species that demonstrates broad antioxidant, anti-inflammatory, anticancer, and antinociceptive activities.

An analog of suramin that selectively inhibits P2X1 receptors (pIC50 = 6.3); selectively antagonizes the Gsα-subunit G protein, which suppresses the association rate of GTPγS binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks G protein coupling to…

A quinone derivative that inhibits red blood cell PLA2 with a Ki value of 130 µM.

A succinimide that is converted to N-desmethylmethosuximide, a channel blocker that targets low threshold calcium currents; inhibits CYP2C19-mediated metabolism of biguanides; has anticonvulsant properties in clinical trials.

A potent inhibitor of specific IAPs that binds baculovirus IAP repeat (BIR) domains (Kis = 28, 14, 17, and 43 nM for XIAP BIR3, NL-IAP BIR, BIRC2 (c-IAP1) BIR3, and BIRC3 (c-IAP2) BIR3, respectively); induces activation of caspases, decreasing the viability of cancer cells without affecting normal cells.

An ERβ Selective agonist; exhibits 70-fold higher relative binding affinity for ERβ versus ERα.

A non-lipid agonist of LPA2 (EC₅₀ = 0.10 µM) that is without effect at other LPA receptor subtypes; protects IEC-6 cells against caspase activation and apoptosis following irradiation; increases the survival of mice suffering from hematopoietic acute radiation syndrome after…

A nucleoside analog with antiviral activity, inhibiting thymidine kinases from herpes simplex virus types 1 and 2 with Ki values of 0.14 and 0.95 µM, while blocking green monkey Vero cell thymidine kinase less effectively (Ki = 53 µM).

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,…

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 potent, selective inhibitor of Stearoyl-CoA desaturase 1 that demonstrates IC50 values of 4.5 and 26 nM in mouse and human enzymatic assays, respectively.

A NO donor with a half-life of three hours at 37°C, pH 7.4; liberates two moles of NO per mole of parent compound.

Modified with a carboxylic acid group terminating the C-16 alkyl chain, providing a convenient site for chemical crosslinking.

A conjugated PUFA that induces cell cycle arrest and apoptosis in a variety of cancer cell lines (GI50 = 1-5 µM); increases the production of ROS, leading to oxidative stress that contributes to cytotoxicity.

A selective autotaxin inhibitor (IC50 = 5.7 nM) that has been shown to dose-dependently block thrombin-induced LPA secretion in platelets.

A non-ionic, water-soluble X-ray contrast agent for intravascular administration; can cause acute kidney injury and is used in animal models of contrast-induced nephropathy.

A biotinylated reagent used for the detection and quantification of apurinic/apyrimidinic (AP) sites in damaged DNA; reacts with aldehyde groups formed when reactive oxygen species depurinate DNA, thereby covalently linking biotin to these AP sites.

A potent pan inhibitor of class I catalytic subunits of PI3K, inhibiting p110α, β, δ, and γ with IC50 values of 3, 33, 3, and 75 nM, respectively; inhibits the growth of certain types of cancer cells, and blocks signaling through PI3K to Akt, both in cells and in vivo.

Selectively inhibits ALK1 (IC₅₀ = 46 nM) and ALK2 (IC₅₀ = 32 nM) with >300-fold selectivity over ALK3, ALK6, and VEGF type 2 receptor; inhibits BMP4 signaling with an IC₅₀ value of 152 nM in a functional assay.

A potential metabolite of bimatoprost when administered to animals; potential minor impurity in commercial preparations of bimatoprost.

A substrate for β-galactosidase, the lactose repressor, the galactose-binding protein, the β-methylgalactoside transport system, and thiogalactoside transacetylase.

A powerful effector in both the TetR and revTetR transcriptional regulator systems, binding the Tet repressor 35-fold more strongly than Tet; does not act a general inhibitor of translation and is a poor antibiotic.

A selective inhibitor of PI3Kα that is equipotent against both wild type and several mutant isoforms (IC₅₀s = 4.0-4.8 nM); dose-dependently inhibits the growth of PI3Kα-dependent xenograft tumors in mice, alone or in combination with other kinase inhibitors.

An ATP-competitive Pim-1 kinase inhibitor (IC₅₀ = 50 nM) that displays selectivity over the related kinases, Pim-2 and MEK1/2 (IC₅₀s = >20 µM).

1-Hexadecyl lysophosphatidic acid is an ether analog of LPA containing a hexadecyl group at the sn-1 position. LPA binds to five different GPCRs to mediate a variety of biological responses including cell proliferation, smooth muscle contraction, platelet aggregation, neurite retraction, and cell motility.

An orally available inhibitor of microtubule polymerization (IC₅₀ = ~3 µM) that blocks cell cycling at the G2-M phase, which leads to cell death; cytotoxic to a range of cancer cell lines (IC₅₀s = 9-101 nM) and demonstrates antivascular activity in tumors both in vitro…

An α-glucosidase inhibitor (IC₅₀ = 5.6 µM) that delays the absorption and digestion of dietary polysaccharides by reversibly inhibiting digestive enzymes such as maltase, isomaltase, and sucrase (IC₅₀s = 0.18, 5.2, and 0.37 µM, respectively).

An alkaloid that inhibits the growth of mouse leukemia P388 cells (IC₅₀ = 1.8 μg/ml); binds to and stabilizes the topoisomerase I-DNA binary complex, leading to DNA breakage and cell death (IC₅₀ = 5.07-12.6 μM); selectively inhibits CYP1A1 and CYP1A2 (IC50 = ~6 μM for…

A natural anthocyanidin.

AH 6809 is an EP and DP receptor antagonist with nearly equal affinity for the cloned human EP1, EP2, EP3-III, and DP1 receptors. AH 6809 blocks the PGE2-induced accumulation of cAMP in COS cells transfected with the human EP2 receptor. It also blocks the accumulation of Ca2+ in Xenopus oocytes…