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.

Ampicillin is a ß-lactam antibiotic that displays antibacterial efficacy against both gram negative and gram positive bacteria. Ampicillin inhibits transpeptidase, preventing bacterial cell wall formation.

Features Each vial contains a mixture of standards packaged in amber ampules purged with argon >1 ml provided at the concentration specified in the insert Designed for direct snap and inject use in mass spectrometry applications Ideally suited for method development and as a…

A cell-permeable dye that is cleaved by intracellular esterases, leaving membrane-impermeant calcein, a fluorescent indicator with absorption and emission maxima of 494 and 517 nm, respectively.

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.

Amiloride is a potassium-sparing diuretic that exhibits antihypertensive and antiviral activities. Amiloride inhibits epithelial Na+ channels (ENaCs), acid-sensing ion channels, and Na+/H+ antiporters. Amiloride prevents Na+ reabsorption in the kidney, increasing excretion of Na+ and water; it is…

A quinazoline that inhibits the tyrosine kinase activity of EGFR (IC₅₀ = 0.025 nM); inhibits the growth of SKOV3 and MDA-468 tumor cell lines (EC₅₀s = 6.5 and 30 µM, respectively).

5(S)-HETrE is produced by the action of 5-LO when mead acid is the substrate. There are no literature reports of the biological activity or further metabolic fate of 5(S)-HETrE.

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.

Chlorpromazine is a phenothiazine that exhibits antipsychotic, antidepressant, anxiolytic, neuroprotective, and anticancer chemotherapeutic activities. Chlorpromazine inhibits D1/2/3/4 receptors, 5-HT1/2 receptors, a1/2-adrenergic receptors, and M1/2 muscarinic acetylcholine receptors (mAChRs).…

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 prodrug that is rapidly catabolized in vivo to 5-fluorouracil when administered by rapid injection; inhibits thymidylate synthase (EC₅₀ = 0.6 nM), interfering with DNA synthesis; used to treat various cancers, particularly metastases to the liver.

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.

Anethole trithione is an oltipraz analog that is clinically used to treat xerostomia (dry mouth). Anethole trithione enhances salivary gland secretion.

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).

11β-PGF2α-EA is the theoretical hepatic metabolite of PGD2-EA, produced during COX-2 metabolism of the endogenous cannabinoid AEA which is found in brain, liver, and other mammalian tissues. AEA can be used directly by COX-2 and specific PG synthase to produce ethanolamide congeners of…

An activator of the P2X receptors that exhibits 5-30-fold greater potency at the P2X7 receptor than ATP; activates the human, rat, and mouse receptors with EC₅₀ values of 0.7, 3.6, and 285 μM, respectively.

Aflatoxins are mycotoxins found in foods and livestock feeds that were initially produced by species of Aspergillus. Aflatoxin G2 is cytotoxic; it inhibits DNA synthesis and induces cell cycle arrest.

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.

Atriopeptin III is an analog of atrial natriuretic peptide (ANP) that exhibits vasodilatory/hypotensive and diuretic activities. In rat kidneys, atriopeptin III increases the diameter of constricted afferent arterioles, decreasing blood pressure.

A short chain fatty acid that inhibits HDACs, induces growth arrest, differentiation and apoptosis in cancer cells, and suppresses inflammation by reducing the expression of pro-inflammatory cytokines.

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 common C-12 saturated far plentiful in coconut and other nut oils.

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…