A nucleoside reverse transcriptase inhibitor that, following triphosphorylation by thymidine kinase, potently blocks replication of HIV (EC₅₀ = 3 nM) with low cytotoxicity (CC50 > 5 μM).

The primary metabolite of mycophenolic acid, an inhibitor of inosine monophosphate dehydrogenase that prevents lymphocyte proliferation and activation; typically used as an internal standard for therapeutic drug monitoring analyses of serum or whole blood by HPLC or LC-MS to confirm that patients…

An isoflavonoid phytoestrogenic compound found in soybeans, pea pods, and other legumes; acts as a tyrosine kinase inhibitor, has chemopreventive effects on breast, prostate, and other endocrine-dependent tumors.

A benzoxazolone derivative that causes skeletal muscle relaxation and blocks spasticity in clinical studies; enhances KCa2.2 and KCa3.1 channels (EC₅₀s = 87 and 98 µM, respectively); urinary excretion of its 6-hydroxy metabolite is often used as a probe of CYP2E1 activity in…

GSK2578215A is a potent inhibitor of leucine-rich repeat kinase 2 (LRRK2; IC₅₀ = 8.9 nM) that also inhibits the G2019S mutant of LRRK2 (IC₅₀ = 10.1 nM). It displays selectivity for LRRK2 over a panel of 460 other kinases. GSK2578215A prevents phosphorylation of both wild-type…

A fluorogenic substrate of palmitoyl-protein thioesterase.

A hepatotoxic monocylic pentapeptide that acts as a potent inhibitor of protein phosphatase types 1 (PP1) and 2A (PP2A), exhibiting IC50 values of 1.8 and 0.026 nM, respectively.

Commonly used as a pH indicator, a color marker in agarose or polyacrylamide gel electrophoresis, and a dye to detect proteins and nucleic acids (absorbance at 610 nm), particularly when staining living tissues.

N-(4-Carbethoxyphenyl)retinamide is a retinoid that exhibits anticancer chemotherapeutic and chemopreventive activities. This compound inhibits development of stomach and oral cancers in vivo and shows some benefit in the treatment of dysplasias. Additionally, this compound induces differentiation…

A selective allosteric inhibitor of Bcr-Abl (IC₅₀s = 4.52, 0.38, and 0.93 µM against Bcr-Abl mutants G250E, E255V, and M351T, respectively); displays additive inhibitory activity against T315I Bcr-Abl mutants both in in vitro assays and in a recalcitrant T315I Bcr-Abl mutant mouse…

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

20-HETE is a major biologically active CYP450 metabolite of arachidonic acid in the kidney and liver. It regulates renal vascular and tubular functions as well as vascular tone in the cerebral circulation. HET0016 is an inhibitor of 20-HETE formation in human renal microsomes with an…

A potent marine-derived neurotoxin that reversibly inhibits the inward sodium current through NaV channels (IC₅₀s = 4.1 and 5.2 nM, respectively, in frog muscle and squid axon; Kd = 1.8 nM in rat brain), blocking nerve and muscle action potentials.

β-Gal-NONOate is a nitric oxide (NO) donor which releases NO following activation by β-galactosidase. β-Gal-NONOate is stabile in aqueous solution at neutral and acidic pH for several hours, exhibits good water solubility, and is able to cross the cell membrane. Following enzymatic…

Steroisomer of PGF1α with both C-9 and C-11 hydroxyls inverted.

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…

A naturally occurring plant hormone of the auxin class that stimulates cell elongation and division, promoting plant growth and development.

Aflatoxins are mycotoxins found in foods and livestock feeds that were initially produced by species of Aspergillus. Aflatoxin G1 is cytotoxic; it inhibits DNA synthesis and induces cell cycle arrest.

A major metabolite of PGD2 found in human and mouse urine at levels of approximately 1.5 and 8.1 ng/mg creatinine, respectively.

A potent ER antagonist that works by both down-regulating and degrading ERα; efficacious in the treatment of estrogen-sensitive breast cancer; fully activates ER on hippocampal neurons.

A metabolite of vinclozolin, a dicarboximide fungicide, that acts as an effective antagonist of the androgen receptor (Ki = 9.7 µM in rat).

A synthetic thyroid hormone mimetic that lowers total and LDL cholesterol up to 40% when administered to humans at a dose of 50-200 µg once daily for 14 days; stimulates cholesterol catabolism to bile acids without affecting cholesterol synthesis.

A fluorescently-labeled deoxyglucose analog that is used primarily to directly monitor glucose uptake by living cells and tissues; also used as a topical contrast reagent for the detection of neoplasia.

A lipid peroxidation product derived from oxidized ω-6 PUFAs such as linoleic acid and arachidonic acid which is widely used as a marker of lipid peroxidation.

Anoninvasive, intracellular calcium indicator that is UV light-excitable; spectral properties in the presence of low calcium concentrations (excitation max = 362 nm, emission max = 512 nm) differ from those during high calcium conditions (excitation ma

6-Aminocaproic acid is a protease inhibitor that displays anticancer activity but is limited by cytotoxicity. 6-Aminocaproic acid inhibits plasmin, preventing fibrinolysis; it may exhibit pro-thrombotic activity, as it is clinically used to treat bleeding disorders.

A phospholipid containing the long-chain (14:0) myristic acid inserted at the sn-1 and sn-2 positions.

N-Acetyl-S-(N’-phenylthiocarbamoyl)-L-cysteine (PITC) is a cysteine conjugate of N-acetyl-phenylisothiocyanate. Isothiocyanates are typically found in plants of the Brassicaceae family, including broccoli, cabbage, and radish. Isothiocyanates are best known for their antioxidative, anticancer…

A cell-permeable analog of cGMP that preferentially activates cGMP-dependent protein kinase; 1 µM-0.1 mM inhibits acetylcholine-induced increases in intracellular calcium concentrations.

An inhibitor of p53-HDM-2 interaction that can reactivate the tumor suppressor function of wild-type p53; binds to p53 with an apparent Kd value of 1.5 nM and prevents interaction with HDM-2 resulting in p53 stabilization, accumulation, and activation.

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.

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…