An inhibitor of Cdc7 kinase (IC₅₀ = 10 nM) as well as Cdk9, (IC₅₀ = 34 nM); induces apoptotic cell death in multiple cancer cell types at 10 µM.

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 platinum-containing compound that acts as an alkylating agent; used alone or in combination therapy in the treatment of several types of cancer; inhibits the RecA recombinase of M. tuberculosis (IC₅₀ = 2 µM), blocking protein splicing and cell growth.

A dihydropyridine used as an antihypertensive agent due to its ability to block L-type and T-type calcium channels; also binds to adenosine A₁, A_2A, and A₃ receptors with K_i values of 8.96, 23.0, and 8.3 µM, respectively.

A physiologically active metabolite of losartan; a potent AT1 antagonist (Kis = 0.57 and 0.67 nM for rat and human forms, respectively), producing a depressor response and vasodilatation.

A hybrid molecule patterned after N-arachidonoyl serotonin; inhibits capsaicin-induced TRPV1 channel activation (IC₅₀ = 2.57 μM) without blocking FAAH-mediated hydrolysis of arachidonoyl ethanolamine (IC₅₀ > 50 μM).

A highly potent, reversible inhibitor of the EGFR (Ki = 5.2 pM; IC₅₀ = 29 pM); rapidly suppresses autophosphorylation of EGFR in ?broblasts and human epidermoid carcinoma cells.

A cell permeable drug that inhibits cholesterol trafficking from late endosomes/lysosomes to the ER, but not to the plasma membrane.

An inhibitor of HIF-1α protein translation; suppresses phosphorylation of two key regulators of protein synthesis, eukaryotic translation initiation factor 4E binding protein 1 (4EBP1) and p70 S6 kinase; cytotoxic to a variety of cancer cell lines with an IC₅₀ value of 15-25 µM.

DGLA is a metabolite produced by chain elongation of the essential fatty acid γ-linolenic acid. Ethyl DGLA is an esterified version of the free acid which is less water soluble, but more ammenable for the formulation of DGLA-containing diets and dietary supplements. DGLA has been advanced as…

A cell-permeable, fluorescent probe for DNA that is useful as a marker of nuclei for cell cycle studies in combination with BrdU and to distinguish nuclear morphology in apoptotic cells.

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 skeletal muscle relaxant that has applications in reducing muscle spasm, limitations in normal motion, and pain caused by musculoskeletal conditions.

An inhibitor of both CDK1 and CDK2 (IC₅₀s =2.9 and 2.2 µM, respectively); inhibits cellular ataxia telangiectasia mutated and Rad3-realted kinase activity (IC₅₀ = 6.7 µM) and impairs G2/M arrest in various human cancer cells, potentiating the cytotoxic effects of…

A high-affinity ligand for retinoid X receptors (RXRs)(EC50 = 28, 25, and 20 nM for RXRα, β, and γ, respectively); inhibits cell cycle progression, induces apoptosis, and blocks angiogenesis and metastasis; stimulates clearance of soluble Aβ, reduces plaque area, and reverses…

The defining agonist for the AMPA subgroup of ionotropic glutamate receptors, which mediate excitatory neurotransmission; contains an equal mixture of the active (S)-enantiomer and the inactive (R)-enantiomer.

A small molecule, multi-targeted receptor tyrosine kinase inhibitor; potently inhibits signaling through PDGFR, VEGFR, KIT, and FLT3; inhibits both tumor cell growth and angiogenesis; approved by the FDA for the treatment of gastrointestinal stromal tumor and metastatic renal cell carcinoma.

A nonaminoglycoside that has been reported to selectively induce ribosomes to read through premature nonsense stop signals on mRNA, thus allowing the production of full-length, functional proteins (IC₅₀ = 7 nM); 60 mg/kg s.c. injection or 0.3-0.9 mg/ml orally has been shown to restore…

A potent, orally available inhibitor of CDKs, blocking the Cdk9 activity of P-TEFb (IC50 = 8 nM) as well as all other CDK isoforms (IC50 = 100-300 nM); less effectively inhibits EGFR and PKA (IC50 = 21 and 122 μM, respectively); has potential applications in cancer therapy.

The CysLTs, LTC4 and LTD4, are potent mediators of asthma and hypersensitivity. They induce bronchoconstriction, increase microvascular permeability, and are vasoconstrictors of coronary arteries. Their biological effects are transduced by a pair of GPCRs, CysLT1 and CysLT2. Montelukast (sodium…

An imidazotetrazine that is converted to a compound capable of alkylating DNA, thus interfering with DNA replication and leading to cytotoxicity in proliferating cells; rapidly and completely absorbed from the gastrointestinal tract after oral administration and readily crosses the blood-brain barrier.

A stable, cell-permeable dye employed to assay cell proliferation as it is partitioned with high fidelity between daughter cells for up to eight generational divisions.

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.

A cell-permeable ACL inhibitor (IC₅₀ = 0.13 µM) that has been reported to reduce weight gain and lower plasma cholesterol, triglycerides, and glucose in a mouse model of hyperlipidemia.

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 potent inhibitor of all three human Pim kinases (IC₅₀s = 7, 363, and 69 nM for Pim-1, Pim-2, and Pim-3, respectively); induces apoptosis in lymphocytes from patients with CML or ALL; enhances the activity of sunitinib against renal cell carcinoma and resensitizes chemoresistant cancer…

A potent TRPV1 antagonist that inhibits capsaicin-induced and acid-induced activation of rat TRPV1 with IC50 values of 35 and 6 nM, respectively.

A potent and selective agonist for both LXRα and LXRβ (EC₅₀ = 50 nM).

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, ATP-competitive inhibitor of ROCKs including p160ROCK (Ki = 140 nM) and ROCK-II (IC50 = 800 nM); also inhibits PRK2 with an IC50 value of 600 nM.

A full antagonist of estrogen ERβ receptors with 36-fold selectivity over ERα (relative binding affinities are 0.01 and 0.36, respectively); enhances SKOV3 and OV2008 ovarian cancer cell growth in in vitro assays at 100 pM.

Thiazolidinediones (TZDs) are a group of structurally related PPARγ agonists with anti-diabetic actions in vivo. Rosiglitazone (BRL49653) is a prototypical TZD and has served as a reference compound for this class of PPARγ ligands. Pioglitazone is a closely related TZD which also…