A potent antagonist of the type III receptor tyrosine kinases PDGFRβ, FLT3, and c-Kit (IC₅₀ = 200, 220, and 170 nM, respectively); less potently inhibits CSF-1R (IC₅₀ = 3.4 µM) and does not significantly inhibit other tyrosine or serine/threonine kinases.

An anti-inflammatory steroid.

Norethindrone is a synthetic progestin that possesses antiestrogenic effects, where in low doses it is progestational and in high doses it is antiestrogenic. It also causes a time-dependent loss of cytochrome P-450 when incubated in vitro with rat liver microsomal fractions and NADPH-generating…

An antipsychotic compound that displays high affinity for dopamine receptors (Kis = 2.4, 0.2, and 1.8 nM for D2, D3, and D4, respectively); also has actions as an antagonist, inverse agonist, or channel blocker, with lower affinities, at other receptors and channels.

An organic polysulfide compound found in garlic that acts as an H2S donor; reduces the survival of prostate cancer PC-3 cells (IC50 = 22 μM) and inhibits the growth of human colon adenocarcinoma HCT15 cells (IC50 = 11.5 μM); suppresses the growth of PC-3 xenografts in vivo in mice and induces…

A steroid hormone produced in the cortex of the adrenal glands that binds to both glucocorticoid and mineralocorticoid receptors; also is the precursor to aldosterone synthesis.

Keystone essential fatty acid that is converted by COX, LO, and epoxygenase enzymes into more than 150 potent metabolites in species ranging from fungi to plants to mammals.

Capsaicin is the primary active component of the heat and pain-eliciting lipid-soluble fraction of the Capsicum pepper. Capsaicin is present in natural hot pepper extracts along with a number of impurities, including dihydrocapsaicin and several lesser impurities. Separation by HPLC is required in…

A broad-spectrum nitrofuran antibiotic used against urinary tract infections and as therapy for acute diarrhea of bacterial origin; inhibits the survival and migration of cancer cells, suppressing tumor growth and metastasis in vivo, at least in part by inhibiting STAT3 (IC₅₀ = 10 µM).

A potent dopamine receptor agonist that binds the D2 receptor with highest affinity (Ki = 2.5 nM); avidly binds the serotonin receptors 5-HT1A and 5-HT1D (Ki = 12.9 and 10.7 nM, respectively), as well as α and β adrenoreceptors.

A non-protein amino acid that chelates iron and copper; inhibits certain enzymes that contain iron or copper, including arginase (IC₅₀ = 3.7 µM).

A catatoxic steroid that acts as an agonist of the rodent PXR at µM concentrations; mediates induction of hepatic CYP3A, Oatp2, and Cyp7a1, regulating both xenobiotic and bile acid homeostasis.

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

β-estradiol is a potent mammalian estrogenic hormone produced by the ovary. Triggers the production of gonadotropins leading to ovulation. β-Estradiol is used to study cell differentiation and transformations (tumorigenicity). The pharmacology and HPLC determination of β-Estradiol…

Nicotinic acetylcholine receptor agonist isolated from Nicotiana tabacum and Nicotiana rustica. Nicotine Tartrate finds an application as the nicotine active in a wide range of smoking cessation products such as nicotine lozenges and nicotine sub-lingual tablets. (-)-Nicotine ditartrate is a…

5-Bromotetralone is a synthetic intermediate useful for pharmaceutical synthesis.

Inhibits microtubule polymerization (IC₅₀ =3.2 μM) by binding to tubulin, which disrupts spindle formation during mitosis; blocks the growth of MCF-7 human breast carcinoma cells (IC₅₀ = 13 nM); inhibits neutrophil motility and activity (5 μmol/kg in a mouse model of…

A chromogenic substrate that, like other tetrazolium compounds, can be reduced to produce a colored formazan derivative; used in the “NBT test” to evaluate the activity of NADPH oxidase in phagocytes; paired with PCIB for the colorimetric detection of alkaline phosphatase activity.

A cell-permeable substrate for aminopeptidase M and leucine aminopeptidase that was developed for intracellular analysis of protease activities.

A reversible inhibitor of the H2S synthesizing enzyme cystathionine-γ-lyase; blocks H2S synthesis in rat liver preparations with an IC50 value of 6.5 µM.

An anti-inflammatory compound from the diaryl heterocycle class that selectively inhibits COX-2 (IC50s = 22.9 and 0.05 μM for COX-1 and COX-2, respectively; displays chemopreventive activity in multiple tumor types via proapoptotic effects independent of its capacity to block COX-2.

A natural retinoid that associates with CRBP-I and CRBP-II (Kds = 50 and 90 nM, respectively), which are involved in the intracellular transport of retinol; an intermediate of the phototransduction pathway of photoreceptors; can form toxic conjugates with proteins and lipids, leading to…

Phytochemical from cruciferous vegetables that demonstrates anticancer and chemopreventative effects (10-30 µM) involving the induction of Phase 2 enzymes, promotion of apoptosis, induction of cell cycle arrest, inhibition of cell proliferation, and inhibition of histone deacetylases and DNA…

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.

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 calcium sensitizer that causes increased cardiac contractility by binding troponin C (EC₅₀ = 9 nM), promotes vasodilation by activating ATP-sensitive potassium channels on vascular smooth muscle cells (EC₅₀ = 0.28 µM), and performs a cardioprotective function by…

A selective β-adrenoceptor agonist that shows high affinity for β1, β2, and β3 (Ki = 224, 458, and 1,570 nM, respectively); inhibits contractions in isolated field stimulated rat vas deferens at low concentrations (EC₅₀ = 45.6 nM); increases cAMP levels and can…

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 member of the 2-aryl propionic acid group of NSAIDs that reduces inflammation through inhibition of NF-κB and AP-1 activation; decreases survival of prostate tumor cells by inducing p75NTR protein expression; inhibits the enzyme γ-secretase thereby preventing the formation of the…

A synthetic analog of 2'-deoxy-guanosine which is used to treat or prevent cytomegalovirus (CMV) infections; inhibits the replication of human CMV with an IC₅₀ value of 0.01 μM and is effective against strains of CMV from human, monkey, mouse, and guinea pig.

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.

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).