A dietary flavonoid which has diverse physiological activities through both direct and indirect effects; directly binds ERα and ERβ, acting as an inverse agonist or agonist; acts as an antioxidant; suppresses signaling through certain receptor tyrosine kinases, including EGFR and HGF.

An inhibitor of DNA methyltransferases that reduces hypermethylation associated with certain diseases, including myelodysplastic syndromes (IC50s = 2.4 and 2.6 μM for in vitro anti-myeloma activity) and cancer (IC50s ~ 0.4 μM for inhibiting proliferation of various cancer cell lines).

A quinone which inhibits topoisomerase I at 25 μM and transglutaminase (IC₅₀ = 5 μM); reduced to β-lapachone hydroquinone by NQO1, generating ROS during its reversion to β-lapachone; sensitizes cancer cells to radiation, suppresses NF-κB activation, and drives apoptosis.

A multi-target inhibitor that potently blocks EGFR and HER2 (IC₅₀s = 2.4 and 16.4 nM, respectively) and inhibits the activity of class I and class II HDACs at nanomolar concentrations (e.g., IC₅₀s = 4.5, 12.6, 13.2, and 11.4 nM for HDAC1, 2, 4, and 5, respectively).

A conjugate of biotin and lysine used for derivatization or conjugation to proteins and other molecules with a medium-chain length spacer; also used as an anterograde, retrograde, or intracellular neuroanatomical tracer that is fixable with aldehyde-based fixatives.

A potent and selective agonist for both LXRα and LXRβ (EC₅₀ = 50 nM).

A potent, orally available inhibitor of CDKs, blocking the Cdk9 activity of P-TEFb (IC50 = 8 nM) as well as all other CDK isoforms (IC50 = 100-300 nM); less effectively inhibits EGFR and PKA (IC50 = 21 and 122 μM, respectively); has potential applications in cancer therapy.

An inhibitor of Ras-mediated signaling that inhibits the growth of PANC-1 and U87 tumor cells with IC₅₀ values of 20 and 10 µM, respectively.

An herbicide that is used to control a wide range of terrestrial and aquatic plants.

Zileuton (Zyflo™) is a reversible 5-LO inhibitor that was approved in 1997 for the prevention and treatment of asthma in the USA, but was withdrawn by Abbott Laboratories in 2003. Zileuton inhibits 5-LO from rat basophilic leukemia-1 (RBL-1) cells with an IC50 value of 0.5 µM. It is a…

AMC-AA is one of several fatty acid amides which can be used to measure FAAH activity. Exposure of AMC-AA to FAAH results in the release of the fluorescent aminomethyl coumarin that absorbs at 360 nm and emits at 465 nm, allowing for fast and convenient measurement of FAAH activity using a simple…

Activates cardiac differentiation, inducing the expression of early cardiac genes in mouse pluripotent and embryonic stem cells in vitro at low micromolar concentrations; drives differentiation of human peripheral blood mononuclear cells, mobilized by G-CSF, toward a cardiac phenotype.

An intermediate in the catabolism of aromatic amino acids; formed in excess during alkaptonuria.

A lipophilic, nontoxic, iron-chelating agent that shows high iron chelation efficacy both in vitro in cell culture models and also in vivo in rats and mice.

A carboxylic acid-based inhibitor of aldose reductase (IC₅₀ = 0.01-15 μM) that suppresses high glucose-induced proliferation of vascular smooth muscle cells as well as prevents high glucose-induced intracellular NADH/NAD+ increase and membrane-bound protein kinase C activation.

An L-type calcium channel blocker that is selective over N-, R-, P/Q- and T-type calcium channels; displays antihypertensive activity, lowering arterial blood pressure without altering cardiac contractility.

A fluorescent substrate for calpain and papain (excitation max: 360 nm; emission max: 460 nm) that is used for measuring the chymotrypsin-like peptidase activity of the 20S proteasome.

A powerful effector in both the TetR and revTetR transcriptional regulator systems, binding the Tet repressor 35-fold more strongly than Tet; does not act a general inhibitor of translation and is a poor antibiotic.

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

NAM is a potent, irreversible inhibitor of MAGL or MAGL-like activity in rat cerebellar membranes, exhibiting an IC50 value of 140 nM. Inhibition of MAGL by the sulfhydryl-reactive maleimide group of NAM suggests a critical cysteine residue is present in the substrate-binding site of the enzyme.

A competitive AT1 receptor antagonist (IC50s 1.4 – 3.9 nM and an elimination half-life of 5 to 7 hours) that blocks angiotensin II receptors on both sympathetic nerve terminals and blood vessels.

A glucosamine-nitrosourea which is commonly used to induce experimental diabetes in animals; specifically targets beta cells, entering via the glucose transporter GLUT2 and causing alkylation of DNA, leading to the destruction of beta cells.

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.

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

The major metabolite of the gastric proton pump inhibitor, omeprazole; produced by CYP3A4 sulfoxidation of esomeprazole.

The reduced form of the electron acceptor NADP+ and acts as an electron donor in various biological reactions.

A substrate for the synthesis of RNA during the transcription process and the synthesis of DNA during DNA replication; participates in G-protein-related signal transduction where it is converted to GDP through the action of GTPases.

7-Piperazin-1-yl-thieno[2,3-c] pyridine (hydrochloride) is a synthetic intermediate useful for pharmaceutical synthesis.

A selective inhibitor of PFKFB3 (IC₅₀ = 207 nM); rapidly induces apoptosis in transformed cells, suppresses glucose uptake and growth of Lewis lung carcinomas in syngeneic mice, and yields antitumor effects in human xenograft models of cancer in athymic mice.

A cell-permeable selective inhibitor of the PI3K catalytic subunit p110δ (IC50 = 0.5 μM). It less effectively inhibits p110γ and p110β (IC50 = 29 and 75 μM, respectively) and has no significant effect on p110α and several other kinases.

AZ 5104 is an active, demethylated metabolite of AZD 9291 (Item No. 16237), an irreversible inhibitor of EGFR-sensitizing and T790M resistance mutations (IC₅₀s = 15-17 nM) that spares the wild-type form of the receptor (IC₅₀ = 480 nM). AZ 5104 displays a similar overall…