A Bcr-Abl kinase inhibitor (IC₅₀ = 5.8 nM) that is 25- to 55-fold more potent than imatinib in vitro and ≥10-fold more potent in vivo; inhibits 12 out of the 13 most frequent imatinib-resistant Bcr-Abl point mutations, but not the T315I mutation; also targets the Src family kinase Lyn…

Inhibits smooth MLCK (Ki = 0.3 µM) 10-fold more potently than its parent compound ML-9.

A nonpeptidic antagonist of CCK1 (IC₅₀ = 50 nM) that is 60-fold less effective at CCK2 (IC₅₀ = 3 µM); blocks CCK-mediated gut muscle contraction, pancreatic growth, and pancreatic secretion; commonly used to study the roles of CCK1 in tissues and in animals.

An inhibitor of PLC-dependent processes by an undefined mechanism; inhibits platelet aggregation induced by collagen or thrombin with IC₅₀ values of 0.6 and 5 µM, respectively.

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.

An orally bioavailable inhibitor of Smo; blocks binding of BODIPY cyclopamine (IC₅₀ = 21 nM) and inhibits Gli activation in cell lines that express wild-type Smo or activated mutant forms of Smo (IC₅₀s = 6-35 nM); inhibits Shh pathway activity and prevents tumor growth in…

A metabolite of the nucleoside reverse transcriptase inhibitor, zidovudine, formed by direct conjugation by UGT2B7.

A selective TRPM8 antagonist (IC₅₀s = 8.3 and 5.8 nM in human and rat, respectively); attenuates icilin-induced wet-dog shakes in rats (ED₅₀ = 0.65 mg/kg); reduces HSC3 and HSC4 oral squamous carcinoma cell migration and invasion in vitro.

A derivative of hydrochlorothiazide, which is a diuretic and antihypertensive agent that increases renal excretion of sodium, potassium, chloride, and bicarbonate ions by inhibiting tubular reabsorptive mechanisms.

A potent inhibitor of the TGF-β receptor 1 (TGF-β R1, ALK5) kinase (IC₅₀ = 14.36 nM); blocks TGF-β1-induced phosphorylation and nuclear translocation of SMAD2/3 as well as TGF-β1-directed gene expression; effective in vivo, preventing the development of fibrosis in animals.

A rotenoid compound with chemopreventive and chemosensitizing effects in models of skin, mammary, colon, and lung carcinogenesis; inhibits cell growth (IC50 = 8 M), blocks PI3K/Akt signaling, suppresses COX-2 expression, and induces apoptosis of premalignant and squamous HBE cells without affecting…

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 potent, reversible, ATP-competitive, and selective inhibitor of the Src family of protein tyrosine kinases: p56lck (IC₅₀ = 4 nM), p59fynT (IC₅₀ = 5 nM), Hck (IC₅₀ = 5 nM).

A potent and selective agonist of the human PGE2 receptor, EP4 with a Ki value of 0.38 nM and an EC50 value of 0.6 nM; induces thermal hyperalgesia when injected into guinea pig forepaw and increases vasodilation of human pulmonary vein.

A positive allosteric modulator of the M1 mAChR; dose-dependently reduces the concentration of acetylcholine required to activate M1; the effective range for potentiation is 0.1 to 100 μM with 3 nM acetylcholine; restores impairment in reversal learning in a mouse model of Alzheimer’s disease.

A specific Akt inhibitor that has been shown to inhibit proliferation and to induce apoptosis of thyroid cancer cells (IC₅₀ = 30-60 nM in vitro); inhibits Akt, PDK1, and FLT3 in acute myelogenous leukemia cells, decreasing the colony-forming ability of these cells (IC₅₀…

A cell-permeable bis-indolo (indirubin) compound that acts as a highly potent, selective, reversible, and ATP-competitive inhibitor of GSK3α/β (IC₅₀ = 5 nM); inhibition of GSK activates the Wnt-signaling pathway and sustains pluripotency in human and mouse ESCs; maintains…

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 inactive metabolite of PGE2 formed by 15-hydroxy PGDH PGs inactive.

A tight-binding, allosteric inhibitor of reverse transcriptase that is active against HIV-1 and HIV-2 (both EC₅₀s = 1 nM in vitro).

A homoserine lactone member that possesses a rare odd-numbered acyl carbon chain and may be a minor quorum-sensing signaling molecule in P. aeruginosa strains.

An active metabolite of proguanil, produced by CYP2C19; an inhibitor of dihydrofolate reductase (Kis = 0.3 and 1.5 nM for Plasmodium and human forms, respectively).

A chromogenic substrate that can be cleaved by cathepsin G (Km = 1.7 mM), subtilisins, chymotrypsin (Km = 60 µM), chymase (Km = 4 mM), and cyclophilin; used for inhibitor screening and kinetic analysis.

PGF1β is the C-9 epimer of PGF1α. It was shown to enhance respiratory rate in experimental animals when administered intravenously.

Furegrelate is a potent inhibitor of thromboxane synthase with little effect on other enzymes essential for arachidonate metabolism. The IC₅₀ value is 15 nM for human platelet microsomal thromboxane synthase.

An activated fluorescent molecule (excitation: 494 nm, emission: 519 nm) used for labeling proteins; reacts optimally with sulfhydryl groups on cysteine side chains at pH 7, forming a stable thioether bond.

A potent inhibitor of chymotrypsin and chymase (Ki = 9.36 and 13.1 nM, respectively), that less effectively blocks the activity of cathepsins, papain, and leukocyte elastase.

A corticosteroid prodrug that is converted to its active form, des-CIC, a glucocorticoid receptor agonist (Ki = 0.31 nM); used to ameliorate symptoms of airway inflammatory diseases.

A semisynthetic analog of taxol that inhibits microtubule disassembly (IC50 = 0.2 μM) and inhibits cell replication (IC50 = 0.13 μM); has applications in breast cancer and hormone-refractory prostate cancer; intended for research applications.

3-HPA is an analog of AM404, which is a selective inhibitor of carrier-mediated transport of AEA. 3-HPA is metabolized by both COX-1 and COX-2 and also selectively and irreversibly inhibits COX-2 with an IC50 value of 2 µM.

A selective, short-acting adenosine A2A receptor agonist (Ki = 1.1 nM for pig striatum A2A receptor); used to induce hyperemia, particularly in the context of myocardial perfusion imaging.

An inactive metabolite of artemisinin.