An NMDA open-channel blocker (Ki = 1.2 μM at -60 mV) and uncompetitive antagonist with known anti-Parkinsonian, anti-epileptic, anti-stroke, and anti-Alzheimer’s disease properties; 12 μM blocks 90% of NMDA receptor activity and prevents NMDA-receptor mediated neurotoxicity in rat…

A selective L-type calcium channel blocker with long-acting antihypertensive activity; relaxes depolarization-induced contractions of rabbit aorta (EC₅₀ = 1.4 nM) and reduces the rate of spontaneously beating guinea pig right atria (EC₂₅ = 0.45 nM); attenuates β-amyloid…

A non-cholestatic regioisomer of E217G that acts as a substrate for MRP2, competing with E217G for MRP2-mediated transport (IC₅₀ = 14.2 µM).

A major oxysterol formed from cholesterol by CYP3A4/5; used as a marker for CYP3A4/5 activity.

A dual antagonist of TP and EP4 receptors; inhibits TxA2-induced platelet aggregation (IC₅₀ = 0.26 μM) and bronchial smooth muscle contraction; impairs PGE2-mediated relaxation of piglet saphenous vein, suppresses serum-induced proliferation of fibroblasts, and reduces metastasis in a…

A form of PS that contains the abundant long-chain (16:0) palmitic acid inserted at the sn-1 and sn-2 positions; commonly used in the generation of liposomes and other types of artificial membranes.

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.

The four tocopherols (α, β, .delta., and γ) and four tocotrienols (α, β, .delta., and γ) are forms of vitamin E, which is known for its antioxidant activity. Tocotrienols are found at high concentrations in palm oil and rice bran. Recent studies show tocotrienols…

Mn(III)TBAP is a cell-permeable SOD mimic. At a concentration of 30 µM, it decreases the doubling time of SOD-null E. coli. by 2-fold.

A selective, reversible, and ATP-competitive inhibitor of the ATPase p97 (Ki = 3.2 μM; IC₅₀ = 1.5 μM); blocks endoplasmic reticulum-associated degradation, impairing the autophagy pathway and promoting the activation of caspase-3 and -7 in cancer cells.

A potent inhibitor of DGAT-1 (IC50s = 7 and 24 nM, for human and mouse, respectively); confers significant weight loss within seven days and significantly reduces plasma and liver triglycerides when administered at 3 mg/kg to DIO mice.

A non-symmetrically substituted indolylmaleimide that increases β-catenin levels by inhibiting GSK3β (IC₅₀ = 53 nM); reduces proliferation and increases differentiation of a ReNCell VM cell line derived from human ventral midbrain.

CLA refers to a family of 8 geometric isomers of linoleic acid in which the two double bonds are contiguous. (The predominant form of linoleic acid in nature, 18:ω6, has double bonds at 9 and 12, interrupted by a methylene carbon.) CLA is found in both meat and dairy products, but it is not…

An orally available inhibitor of SGLT1 and SGLT2 (IC₅₀s = 36 and 1.8 nM, respectively, for human isoforms in vitro); improves glycemic control in nonobese diabetes prone mice with type 1 diabetes and in patients with type 2 diabetes in a randomized, placebo-controlled clinical trial.

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

An inhibitor of the initiation of translation that blocks the interaction of eIF4G with eIF4E (KD = 25 μM); prevents the expression of oncogenic proteins in mammalian cancer cells, leading to apoptosis; blocks translation in some viruses that do not require eIF4E or a cap structure for initiation.

A form of the myristic acid that is found in the lipid A component of some Gram negative bacteria, including Escherichia, Haemophilus, Actinobacillus, and Campylobacter species.

A plant alkaloid that demonstrates cytotoxicity against leukemia P-388 cells (IC₅₀ = 2.3 µM) through a mechanism that involves stabilizing the DNA topoisomerase I-DNA complex.

A small molecule inhibitor of nucleophosmin dimers that can prevent cell proliferation and induce apoptosis in various cancer cell lines (IC₅₀s = 1.4-4 µM).

An analog of SB203580, the highly specific pyridinylimidazole inhibitor of p38 MAPK; inhibits IL-1 production in the human monocytic cell line THP (IC50 = 0.20 µM) and binds CSAID binding protein, a serine/threonine kinase homologous to p38, inhibiting its kinase activity (IC50 = 0.03 µM).

A symmetric bis-glycolamide that inhibits the eIF2α phosphorylation-mediated unfolded protein response (IC₅₀ = 5 nM in a cell-reporter assay); passes through the blood-brain barrier and significantly enhances learning and memory in mice and rats.

A glutamine analog that inhibits glutaminases (Ki = 6 µM) and other glutamine-utilizing enzymes, including cytidine triphosphate synthase.

A potent inhibitor of serotonin and norepinephrine reuptake (Kis = 4.6 and 15.6 nM, respectively, for rat synaptosomes); less effectively inhibits dopamine reuptake (Ki = 369 nM); effective in cells, tissues, and in vivo.

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.

A selective inhibitor of STAT3 activation, dimerization and nuclear translocation (IC₅₀ = 5.1 μM at 37°C); 10 μM induces apoptosis in STAT3-dependent breast cancer cells.

A water-soluble receptor antagonist which targets both AMPA- and kainate-sensitive glutamate receptors (IC₅₀ = 0.15 and 4.8 µM, respectively); does not block the NMDA-sensitive glutamate receptor (IC₅₀ = ≥ 90 µM).

A post-synaptic α1-adrenergic receptor antagonist commonly used to improve lower urinary tract symptoms associated with benign prostatic hyperplasia; displays high-affinity with non-selectivity for the three known human α1 adrenoceptors (pKi = 8.0, 8.0, and 8.5 for α1A, α1B,…

A potent inhibitor of autotaxin (IC50 = 2.8 nM in an in vitro enzyme assay); at 30 mg/kg, reduces LPA production by >95% following carrageenan-induced inflammation in rats and inhibits autotaxin activity in human whole blood (IC50 = 101 nM).

A dual inhibitor of c-Src and Abl (IC50 = 2.7 and 30 nM, respectively); less effectively inhibits other kinases; blocks cell motility, migration, adhesion, invasion, proliferation, differentiation, and survival; reduces osteoclast bone resorption.

Raclopride is a selective dopamine D₂/D₃ receptor antagonist with K_i values of 1.8, 3.5, 2,400, and 18,000 nM for D₂, D₃, D₄, and D₁ receptors, respectively. It passes the blood brain barrier and can be used in in vivo…

A neuroexcitatory amino acid that functions as a NMDA and metabotropic glutamate receptor agonist; used to induce brain lesions in animal models of cognitive dysfunction.

A broad spectrum tyrosine kinase inhibitor that blocks angiogenesis through its actions on VEGFR isoforms; has low nanomolar efficacy against VEGFR1 (FLT1), VEGFR2, VEGFR3 (FLT4), and KIT, as well as CSF1R, PDGFRA, and PDGFRB; effective in vivo and useful in the management of certain types of cancer.