A synthetic peptide that contains the sequence PVPPR, which corresponds to a region within human Sos1 that interacts with an SH3 domain of Grb2; specifically blocks the interaction of Sos1 with Grb2, preventing an interaction that is essential for Ras activation by receptor tyrosine kinases.

A potent and selective CB1 receptor inverse agonist (Ki = 243 nM; EC50 = 195 nM); a 10 µM concentration results in 100% and 35% displacement of [3H]-CP-55,940 at the CB1 and CB2 receptors, respectively.

Pure Canavalia ensiformis lectin (Con A) from Jackbean. Isolated by affinity chromatography on cross-linked dextran. Con A exists as a dimer below pH 5.0 and and at pH >7 it exists as a tetramer. Con-A is not a glycoprotein. The monomeric molecular weight of Con-A is 25,500. Con-A does not…

A potent disruptor of microtubules used as a chemotherapeutic compound; inhibits growth of cervical (HeLa), lung (A549), breast (MCF-7), colon (HT-29), ovarian (OVG-1), and pancreatic (PC-Sh) carcinomas with IC50 values ranging from 2.5-7.5 nM; induces mitotic arrest and initiates apoptosis of…

An antibiotic that suppresses the expression of ODC, COX-2, and iNOS at concentrations as low as 0.3 μM and exhibits an anti-metastasis effect and anti-tumor promoter activity in various carcinogenesis mouse models.

An analog of folic acid and aminopterin that is used in the treatment of cancer, autoimmune diseases, ectopic pregnancy, and for the induction of medical abortions; induces adenosine release, inhibits the metabolism of folic acid, and blocks key enzymes in the synthesis of purines and pyrimidines…

Carvedilol phosphate is a cardioprotective a1- and ß1/2-adrenergic receptor inhibitor used to treat congestive heart failure; its inhibitory action at adrenergic receptors slows heart rhythm, decreasing force, pressure, and cardiac workload. Carvedilol phosphate also inhibits release of…

A selective inhibitor of the TGF-β type1 receptor ALK5 (IC₅₀s = 4, 18, and 23 nM for ALK5 autophosphorylation, TGF-β cellular assay, and ALK5 binding in HepG2 cells, respectively); used to induce stem cell pluripotency by replacing the reprogramming transcription factor Sox2…

Aflatoxins are mycotoxins found in foods and livestock feeds that were initially produced by species of Aspergillus. Aflatoxin B2 is cytotoxic; it inhibits DNA synthesis and induces cell cycle arrest.

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 potent blocker of small conductance Ca2+-activated K+ (SK, KCa2) channels that is more effective at SK2 than SK1 and SK3 (IC₅₀ values are 0.06-0.4, 1-12, and 1-13 nM, respectively); ineffective against SK4 at 1 µM.

An alkaloid that inhibits the growth of mouse leukemia P388 cells (IC₅₀ = 1.8 μg/ml); binds to and stabilizes the topoisomerase I-DNA binary complex, leading to DNA breakage and cell death (IC₅₀ = 5.07-12.6 μM); selectively inhibits CYP1A1 and CYP1A2 (IC₅₀ =…

A natural type B trichothecene produced by certain species of the fungus Fusarium; inhibits protein biosynthesis, binds to peptidyl transferase, and inhibits the synthesis of RNA and DNA; passes the blood-brain barrier at different rates in different animals.

An agonist of β-adrenergic receptors that activates the β1, β2, and β3 receptors with pEC₅₀ values of 7.5, 9.0, and 6.8 respectively; displays high selectivity for β-adrenoceptors in the trachea over those in atria; activity is retained in the airway for extended periods.

A potent ATP-competitive inhibitor of ATM kinase (IC₅₀ = 13 nM; Ki = 2.2 nM); sensitizes cells to both ionizing radiation and chemotherapeutic agents; induces senescent breast, lung, and colon carcinoma cells to undergo cell death; inhibits HIV-1 replication in C8166 human T-lymophocyte…

An intermediate in several metabolic pathways, including glycolysis and gluconeogenesis.

A CYP2C9 metabolite of the NSAID diclofenac that demonstrates anti-inflammatory and analgesic properties by inhibiting COX and suppressing PGE2 synthesis.

A natural and potent inhibitor of NEP and NEP2, with Ki values of 2 nM for both enzymes; also a weak inhibitor of the related zinc metalloprotease ECE (Ki = 3.5 µM); has little or no effect on a variety of other proteases.

An analog of ceramide that inhibits alkaline ceramidase (IC50 ~5 µM); suppresses growth of HL-60 cancer cells in culture.

A selective, irreversible inhibitor of IL-1b converting enzyme (ICE; Caspase-1); neuroprotective in a rat model of cerebral ischemia.

The racemic version of a CYP450 metabolite of arachidonic acid that dose-dependently stimulates vasodilation of the rabbit kidney.

A protein cross-linking agent isolated from G. jasminoides Ellis; inhibits UCP2 activity; 5 µM genipin increases glucose-stimulated insulin secretion in isolated pancreatic islets chronically exposed to high levels of glucose; induces apoptosis in FaO rat hepatoma cells and human…

An isoflavonoid phytoestrogenic compound found in soybeans, pea pods, clover, kudzu, and other legumes.

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 potent inhibitor of HCV infection (EC₅₀ = 17 nM) that displays low cytotoxicity of virally-infected human hepatoma Huh7.5.1 cells (CC₅₀ = 21.3 µM); displays good pharmacokinetics in mice when delivered intraperitoneally, with preferential liver distribution without…

A selective serotonin reuptake inhibitor (Ki = 6.2 nM in rat hypothalamus) with comparatively little effect on noradrenaline reuptake (Ki = 1,100 nM); potentiates the pharmacological effects of serotonin and its precursor, 5-hydroxy tryptophan, in the CNS resulting in antidepressant effects.

A selective and irreversible inhibitor of the gastric H+/K+ ATPase pump (IC₅₀ = 1.1 μM).

A serotonin 5-HT1B and 5-HT1D receptor agonist (IC₅₀s = 9.3 and 7.3 nM, respectively) that also has affinity for the 5-HT1F receptor (IC₅₀ = 17.8 nM); constricts human middle meningeal arteries (EC₅₀ = 89.9 nM) and reduces vascular inflammation associated with migraines.

A natural plant sterol that can be isolated from certain seed oils and herbs, including those used for therapeutic purposes.

An acetylated form of L-carnitine that facilitates the uptake of acetyl CoA into mitochondria during fatty acid oxidation, enhances acetylcholine production, and stimulates protein and membrane phospholipid synthesis.

Adrenorphin is an endogenous opioid peptide produced from cleavage of proenkephalin A. Adrenorphin acts as an agonist at ?-opioid receptors (?ORs) and µ-opioid receptors (µORs). Like other opioids, adrenorphin exhibits analgesic, antinociceptive, and gastrointestinal motility modulating…

An internal standard for the quantification of trans-resveratrol by GC- or LC-MS.