A potent, orally bioavailable, ATP-competitive small-molecule dual inhibitor of c-MET (IC₅₀ = 8 nM) and ALK (IC₅₀ = 20 nM) receptor tyrosine kinases; shows antitumor efficacy in multiple tumor models implanted in athymic mice that express activated c-MET or ALK fusion proteins…

AH 6809 is an EP and DP receptor antagonist with nearly equal affinity for the cloned human EP1, EP2, EP3-III, and DP1 receptors. AH 6809 blocks the PGE2-induced accumulation of cAMP in COS cells transfected with the human EP2 receptor. It also blocks the accumulation of Ca2+ in Xenopus oocytes…

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 thiazolidinone that selectively blocks the CFTR channel (Ki = 300 nM) in a voltage-independent manner; prevents cholera toxin-induced fluid secretion in the small intestine, when given by intraperitoneal injection; can affect intracellular GSH concentration and ROS balance.

2-Hydroxymyristic acid is an inhibitor of protein myristoylation requiring about 0.5 mM concentration for full inhibition of acylation.

A calcimimetic compound that can allosterically activate or positively modulate the human CaSR; dose-dependently decreases circulating levels of PTH in both normal individuals and patients with primary hyperparathyroidism in clinical trials.

A long-acting, selective β2-adrenergic agonist with bronchodilator actions (EC₅₀ = 0.25 µM) that demonstrates 2,818-fold selectivity for β2-adrenergic receptors over β1-adrenergic receptors.

An irreversible inhibitor of ornithine decarboxylase that suppresses polyamine biosynthesis; displays antiangiogenic, cytostatic, and antiparasitic effects.

A lipoic acid analog that inhibits α-ketoglutarate dehydrogenase, particularly in tumor cells; induces a strong mitochondrial burst of reactive oxygen species at 60-240 µM, resulting in cell death; demonstrates both in vitro and in vivo anti-tumor activity.

A competitive antagonist of muscarinic receptors that potently blocks signaling through M1, M2, and M3 (Kis = 25, 125, and 10 nM, respectively), resulting in muscle relaxation.

A cell-permeable, stable free radical that is commonly used to evaluate the ability of compounds to act as free radical scavengers or hydrogen donors and to measure the antioxidant activity of tissue extracts; followed by color change from purple (absorbance at 515-528 nm) to yellow.

An inhibitor of DPP-4 (IC₅₀ = 3.5-34 nM); also inhibits DPP-8 and DPP-9 (Ki = 810 and 95 nM, respectively) but not DPP-2 or FAPα; blocks the degradation of several circulating peptides, including incretins; reduces fasting and postprandial glucose levels and decreases inflammatory…

A nitrogen mustard β-chloro-nitrosourea compound used as an alkylating agent to form interstrand crosslinks in DNA, which leads to cancer cell cytotoxity and apoptosis; also reported to inhibit glutathione reductase, thioredoxin reductase, and lipoamide dehydrogenase.

A 2' deoxy analog of 5-azacytidine which is incorporated into DNA and causes hypomethylation by inhibiting DNA methyltransferases in a concentration-dependent manner; useful in conditions characterized by DNA hypermethylation, as is found in myelodysplastic syndromes.

A positive modulator of the small conductance calcium-activated potassium channels SK2 and SK3 (EC₅₀s = 14 and 5.6 µM, respectively); inactive on both SK1 and IK; increases the apparent calcium-sensitivity of channel activation of SK3, changing the EC₅₀ value of calcium…

A natural triterpenoid carboxylic acid that is known to have antioxidative, antimicrobial, anti-inflammatory, and anticancer activities; inhibits Na+/K+-ATPase activity (IC50 = 24.7 μM) and blocks NF-κB activation in various human cancer cells lines (10-100 μM), inhibiting cell…

A selective, cell-permeable EZH2 inhibitor (IC₅₀ = 2 nM) that has been shown to inhibit H3K27methylation in MCF10A cells with an IC₅₀ value of 124 nM.

A plant hormone with diverse roles in disease resistance, plant development, and response to stresses; regulates gene expression and may contribute to epigenetic changes at the chromatin level.

2-(hydroxymethyl)-Pyrimidine is a synthetic intermediate useful for pharmaceutical synthesis.

A broad-spectrum tetracycline antibiotic which has a particularly long half-life in serum; commonly used in the treatment of acne in older patients; also has both anti-inflammatory and neuroprotective actions.

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.

A potent and selective PPARγ ligand. It binds to the PPARγ ligand-binding domain with a Kd of 43 nM.

3-Tert-butyl-4-hydroxyanisole (3-BHA) is one component of butylated hydroxyanisole (BHA). This compound is commonly used as a food additive; it exhibits antioxidative and anticancer activities. In leukemia cells, 3-BHA decreases the mitochondrial membrane potential, inhibits mitochondrial oxidative…

Cisplatin is a platinum-based cross-linking agent that exhibits anticancer chemotherapeutic activity. Cisplatin induces crosslinks between guanine bases on DNA; it is clinically used to treat various forms of cancer. In lung cancer cells, cisplatin decreases phosphorylation of PI3K, Akt, and FOXO3a…

A water soluble, irreversible, broad spectrum inhibitor of serine proteases, including trypsin, chymotrypsin, plasmin, thrombin, and kallikreins; also inhibits NADPH oxidase.

A reversible, selective, allosteric antagonist of mGluR7 that blocks agonist-induced calcium mobilization (IC₅₀ = 26 nM).

An N-hydroxysuccinimide ester of the nitroxide spin label tempyo; an active acylating agent that preferentially targets α-amino groups, used to spin label proteins and aminoacylated RNA species.

An HNF4α antagonist that can repress the expression of known HNF4α target genes, inhibiting endogenous insulin expression in vitro (IC50 = 930 nM).

A natural alkaloid that acts as a selective and reversible α2-adrenergic receptor antagonist (Ki = 12 nM); also acts as a receptor antagonist at the serotonin 5-HT2B receptor (Ki = 14.3 nM).

A glutamine analog that inhibits glutaminases (Ki = 6 µM) and other glutamine-utilizing enzymes, including cytidine triphosphate synthase.

A quinazolinone derivative that selectively inhibits dynamin GTPase activity in yeast and mammalian cells (IC₅₀ = 1-10 μM); prevents apoptosis by inhibiting mitochondrial outer membrane permeabilization.

A derivative of fluphenazine that contains an alkylating chlorethylamine chain, which produces irreversible protein binding; a relatively selective, irreversible antagonist of D2 receptors both in vitro (IC₅₀ = 100 nM) and in vivo; irreversibly inhibits calmodulin at higher doses…