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 selective inhibitor of NUAK1 (IC₅₀ = 100 nM); partially inhibits the phosphorylation of the NUAK1 substrate MYPT1 at Ser445; inhibits proliferation and migration of mouse embryonic fibroblasts and U2OS cells at 10 µM in cell-based assays.

A selective, ATP-competitive inhibitor of the serine/threonine kinase, glycogen synthase kinase 3β (Ki = 38 nM; IC₅₀ = 104 nM); demonstrates neuroprotective effects by inhibiting tau phosphorylation (IC₅₀ = 2.7 μM) at a GSK3-specific site (Ser396) in cells stably…

A Hsp90 inhibitor (IC50 = 21 nM in a FP binding assay) that prevents the proliferation of a range of human cancer cell lines in vitro (GI50s ~ 9nM); 50 mg/kg inhibits tumor growth in a human colon cancer xenograft model by ~50% compared to vehicle controls.

An inhibitor of p53-HDM-2 interaction that can reactivate the tumor suppressor function of wild-type p53; binds to p53 with an apparent Kd value of 1.5 nM and prevents interaction with HDM-2 resulting in p53 stabilization, accumulation, and activation.

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

6-keto prostaglandin F_1α (6-keto PGF_1α) is the inactive, non-enzymatic hydrolysis product of PGI₂. 6-keto PGF_1α serves as a useful marker of PGI₂ biosynthesis in vivo. When [ 3 H]-PGI₂ is injected into healthy human…

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

A major metabolite produced from testosterone by the actions of CYP3A4 and CYP3A5.

Inhibits several isoforms of protein kinase C (PKC; IC₅₀ = 7, 7, 6, 10, 60, and 20,000 nM for PKCα, PKCβ, PKCγ, PKCδ, PKCζ, and PKCμ, respectively); provides cardioprotective effects in myocardial ischemia/reperfusion.

A fluorescent molecule that can be used to detect cholesterol by fluorescence and freeze-fracture electron microscopy.

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 naturally occurring diterpene that directly activates adenylyl cyclase to raise levels of cAMP in a wide variety of cell types; binds to type 1 adenylyl cyclase membranes with an IC50 value of 41 nM and demonstrates an EC50 value of 0.5 μM in an activation assay.

A bifunctional photoreactive agent for crosslinking nucleic acids; intercalates into double-stranded regions in DNA or RNA and, upon UV irradiation, forms covalent adducts with pyrimidine bases; used to study different types of RNA from diverse organisms, including viruses.

A cell-permeable selective inhibitor of the PI3K catalytic subunit p110δ (IC50 = 0.5 μM). It less effectively inhibits p110γ and p110β (IC50 = 29 and 75 μM, respectively) and has no significant effect on p110α and several other kinases.

A competitive inhibitor of 15-hydroxy PGDH; acts as an agonist on most EP receptor subtypes (Kd d~ 1 nM for isolated EP2 receptors); preserves the self-renewal properties while preventing the differentiation of hematopoietic stem cells during expansion in culture.

A dual inhibitor of COX and LOX pathways, that decreases levels of PGE2, LTB4, and lipoxins and prevents LPS-stimulated IL-1β expression.

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…

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 small molecule inhibitor of MDMX.

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.

The peroxisome proliferator-activated receptor γ (PPARγ) is the nuclear receptor responsible for transducing the therapeutic activity of the thiazolidinediones. Thiazolidinediones are a group of structurally related synthetic PPARγ agonists with antidiabetic actions in vivo.…

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 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 substrate for polyamine oxidase that is oxidized to 3-acetamidopropanal and putrescine, a polyamine involved in the division, differentiation, and membrane function of cells; used to examine the interaction between DNA and polyamines during the cleavage of phosphodiester bonds at…

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

A lysyl amide prodrug of the benzothiazole 5-fluoro 203, a high affinity AhR ligand that elicits antitumor activity by inducing transcription of CYP1A1, which leads to the formation of DNA adducts and cell cycle arrest.

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

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.

One of the phenolic antioxidants present in extracts of rosemary; inhibits the formation of tumors derived using irritants such as TPA and DMBA.