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

A major oxysterol formed from cholesterol by CYP3A4/5; used as a marker for CYP3A4/5 activity.

An analog of geldanamycin which has potent in vivo activity and reduced toxicity; has diverse anti-tumor actions; promotes the degradation of HER2 and induces growth arrest and apoptosis in breast cancer cells overexpressing HER2 (IC50 = 4-72 nM).

Bicyclo PGE2 is a stable, base-catalyzed transformation product of 13,14-dihydro-15-keto PGE2. 13,14-dihydro-15-keto PGE2 itself is a metabolite of PGE2 found in human plasma at a median level of 20-25 pg/ml. Due to the inherent instability of 13,14-dihydro-15-keto PGE2, it is advisable to quantify…

Initiates glycogen synthesis in hepatocytes by causing inactivation of phosphorylase a and activation of glycogen synthase a (maximal effects with ~20 µM Itu); potent inhibitor of ERK2 (Ki = 525 nM).

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…

Reversibly inhibits dihyroorotate dehydrogenase, the rate-limiting step in the de novo synthesis of pyrimidines, preventing DNA synthesis of activated lymphocytes (IC₅₀s = 0.09, 3.5, and 12.5 μM for rat, mouse, and human, respectively); also inhibits tyrosine kinases responsible for…

A phosphonic analog of ATP and agonist of P2X1 and P2X3 (EC50 = ~1 µM); ~1,000-fold less potent at P2X2, P2X receptors 4-7, and P2Y receptors; used as a stable analog of ATP to study the interaction of ATP with kinases and other proteins.

An orally active inhibitor of PI3Kg that suppresses joint inflammation in mouse models of rheumatoid arthritis; inhibits human recombinant PI3Kg, a, b, and d in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively.

2-O-ethyl PAF C-16 is a synthetic PAF analog which contains an ethyl group, attached by an ether linkage, at the sn-2 position. It is a less potent agonist than methylcarbamyl PAF C-16 in the induction of platelet aggregation in both human and rabbit PRP. 2-O-ethyl PAF C-16 causes aggregation of…

An agonist for mCAR (EC₅₀ = 20 nM) that is effective for the mouse receptor but not for human or rat CAR receptors; potently induces cytochrome P450 monooxygenases and multidrug resistance and xenobiotic efflux proteins.

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 and selective inhibitor of reticulocyte 15-LO-1.

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…

A γ-secretase inhibitor that blocks Notch processing (IC₅₀ = 1.7 nM); reduces Aβ40 levels by 71% in an APP transgenic mouse model within 4 hours after a single 100 μM/kg dose.

DPI is an irreversible inhibitor of iNOS and eNOS with IC₅₀ values of 50 nM and 0.3 µM, respectively. This inhibition is potent, irreversible, and time and temperature dependent. NADPH, NADP+, and 2'5'-ADP block the inhibitory action of DPI. Similarly, FAD or FMN protect…

A panaxadiol that has diverse in vitro and in vivo effects, including anti-cancer, neuroprotective, anti-hypertensive, and anti-inflammatory actions; induces apoptosis and inhibits angiogenesis in a variety of cancer models.

A cell permeable drug that inhibits cholesterol trafficking from late endosomes/lysosomes to the ER, but not to the plasma membrane.

A product of CYP2A6 metabolism of the primary nicotine metabolite, cotinine; as a biomarker of nicotine metabolism.

A selective calcium ionophore that mobilizes intracellular calcium stores. It is used as a research tool to raise the intracellular level of calcium, to study calcium transport across biological membranes, and to stimulate the intracellular production of cytokines.

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.

A reactive disulfide-containing, fluorescent probe designed to detect H2S in biological samples and cells.

GSK2126458 is a potent inhibitor of phosphoinositide 3-kinase isoforms (K_is = 19, 130, 24, and 60 pM for p110α, β, δ, and γ, respectively). It also inhibits mTOR in both mTORC1 and mTORC2 (K_is = 180 and 300 nM, respectively), as well as several common…

An intermediate in the HMG-CoA reductase pathway derived directly from farnesyl pyrophosphate and used in the biosynthesis of terpenes and terpenoids; also serves as a substrate in the prenylation of a variety of critical intracellular proteins including small GTPases.

A analog of tenovin-1; elevates p53 activity in MCF-7 cells at 10 µM and reduces growth of ARN8 melanoma xenograft tumors in SCID mice at a dose of 50 mg/kg.

A mycotoxin produced in food and animal feeds; activates estrogen receptors, alters hormone levels, and hasten pre-pubertal development; can cause uterine, rectal, and vaginal prolapse, abortion, and infertility in older animals.

An internal standard for the quantification of (±)-β-hydroxybutyrate (sodium salt) by GC- or LC-MS.

A selective, reversible inhibitor of vacuolar H+-ATPases (V-ATPases), blocking these proton pumps in mammalian, plant, or fungal cells with an IC50 value in the 4-400 nM range; also inhibits autophagy by preventing vacuolar acidification necessary for autophagosome maturation.

A sulfated form of taurocholic acid that may be involved in the elimination and detoxification of bile acids during hepatobiliary diseases.

Selectively and reversibly blocks MAGL activity (IC₅₀s = 0.18 and 59 µM for MAGL and FAAH in mouse brain, respectively); does not inhibit ABHD6, ABHD12, CB1, or CB2 receptors (Kis > 10 µM); used to ameliorate disease progression in a mouse model of multiple sclerosis.

An active, deacetylated metabolite of T-2 toxin; inhibits protein synthesis and cell proliferation in plants; causes acute and chronic toxic effects in animals that ingest contaminated plant materials.

A benzothiazinone compound that selectively inhibits both MAO-B activity (IC₅₀ = 34.9 nM in human) and adenosine A2A receptors (Ki = 39.5 nM in human); designed as a potential dopamine-sparing therapeutic in the treatment of Parkinson’s disease.